[go: up one dir, main page]
More Web Proxy on the site http://driver.im/ Skip to main content

Advertisement

Springer Nature Link
Log in

Lipid-based emulsion drug delivery systems — a comprehensive review

  • Review Article
  • Published:
Drug Delivery and Translational Research Aims and scope Submit manuscript

Abstract

Lipid-based emulsion system — a subcategory of emulsion technology, has emerged as an enticing option to improve the solubility of the steadily rising water-insoluble candidates. Along with enhancing solubility, additional advantages such as improvement in permeability, protection against pre-systemic metabolism, ease of manufacturing, and easy to scale-up have made lipid-based emulsion technology very popular among academicians and manufacturers. The present article provides a comprehensive review regarding various critical properties of lipid-based emulsion systems, such as microemulsion, nanoemulsion, SMEDDS (self microemulsifying drug delivery system), and SNEDDS (self nanoemulsifying drug delivery system). The present article also explains in detail the similarities and differences between them, the stabilization mechanism, methods of preparation, excipients used to prepare them, and evaluation techniques. Subtle differences between nearly related terminologies such as microemulsion and nanoemulsion, SMEDDS, and SNEDDS are also explained in detail to clarify the basic differences. The present article also gives in-depth information regarding the chemical structure of various lipidic excipients, various possible chemical modifications to modify their inherent properties, and their regulatory status for rational selection.

Graphical abstract

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Subscribe and save

Springer+ Basic
£29.99 /Month
  • Get 10 units per month
  • Download Article/Chapter or eBook
  • 1 Unit = 1 Article or 1 Chapter
  • Cancel anytime
Subscribe now

Buy Now

Price includes VAT (United Kingdom)

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4

Similar content being viewed by others

References

  1. Lipinski CA. Drug-like properties and the causes of poor solubility and poor permeability. J Pharmacol Toxicol Methods. 2000;44:235–49.

    Article  CAS  PubMed  Google Scholar 

  2. Saal C, Petereit AC. Optimizing solubility: kinetic versus thermodynamic solubility temptations and risks. Eur J Pharm Sci. 2012;47:589–95.

    Article  CAS  PubMed  Google Scholar 

  3. Bergström CAS, Luthman K, Artursson P. Accuracy of calculated pH-dependent aqueous drug solubility. Eur J Pharm Sci. 2004;22:387–98.

    Article  PubMed  CAS  Google Scholar 

  4. Murdande SB, Pikal MJ, Shanker RM, Bogner RH. Aqueous solubility of crystalline and amorphous drugs: challenges in measurement. Pharm Dev Technol. 2011;16:187–200.

    Article  CAS  PubMed  Google Scholar 

  5. Ishikawa M, Hashimoto Y. Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry. J Med Chem. 2011;54:1539–54.

    Article  CAS  PubMed  Google Scholar 

  6. Shibata Y, Fujii M, Kokudai M, Noda S, Okada H, Kondoh M, Watanabe Y. Effect of characteristics of compounds on maintenance of an amorphous state in solid dispersion with crospovidone. J Pharm Sci. 2007;96:1537–47.

    Article  CAS  PubMed  Google Scholar 

  7. Takano R, Takata N, Saito R, Furumoto K, Higo S, Hayashi Y, Machida M, Aso Y, Yamashita S. Quantitative analysis of the effect of supersaturation on in vivo drug absorption. Mol Pharm. 2010;7:1431–40.

    Article  CAS  PubMed  Google Scholar 

  8. Tinworth CP, Young RJ. Facts, patterns, and principles in drug discovery: appraising the rule of 5 with measured physicochemical data. J Med Chem. 2020.

  9. Li S, He H, Parthiban LJ, Yin H, Serajuddin AT. IV-IVC considerations in the development of immediate-release oral dosage form. J Pharm Sci. 2005;94:1396–417.

    Article  CAS  PubMed  Google Scholar 

  10. Lipinski C. Poor aqueous solubility—an industry wide problem in drug discovery. Am Pharm Rev. 2002;5:82–5.

    Google Scholar 

  11. Čerpnjak K, Zvonar A, Gašperlin M, Vrečer F. Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs. Acta Pharm. 2013;63:427–45.

    Article  PubMed  CAS  Google Scholar 

  12. Rahman A, Harwansh R, Mirza A, Hussain S, Hussain A. Oral lipid based drug delivery system (LBDDS): formulation, characterization and application: a review. Curr Drug Deliv. 2011;8:330–45.

    Article  CAS  PubMed  Google Scholar 

  13. Kulkarni CV, Mezzenga R, Glatter O. Water-in-oil nanostructured emulsions: towards the structural hierarchy of liquid crystalline materials. Soft Matter. 2010;6:5615–24.

    Article  CAS  Google Scholar 

  14. Kulkarni CV. Lipid crystallization: from self-assembly to hierarchical and biological ordering. Nanoscale. 2012;4:5779–91.

    Article  CAS  PubMed  Google Scholar 

  15. Kulkarni CV, Glatter O. Hierarchically organized systems based on liquid crystalline phases. Wiley Online Library. 2012;157–191.

  16. Sabir F, Qindeel M, Rehman Au, Ahmad NM, Khan GM, Csoka I, Ahmed N. An efficient approach for development and optimization of curcumin loaded solid lipid nanoparticles’ patch for transdermal delivery. J Microencapsul. (2021);1–34.

  17. Hoar TP, Schulman JH. Transparent water-in-oil dispersions: the oleopathic hydro-micelle. Nature. 1943;152:102–3.

    Article  CAS  Google Scholar 

  18. Calvo P, Vila-Jato JL, Alonso MJ. Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules, and nanoemulsions, as ocular drug carriers. J Pharm Sci. 1996;85:530–6.

    Article  CAS  PubMed  Google Scholar 

  19. Anton N, Vandamme TF. Nano-emulsions and micro-emulsions: clarifications of the critical differences. Pharm Res. 2011;28:978–85.

    Article  CAS  PubMed  Google Scholar 

  20. McClements DJ. Nanoemulsions versus microemulsions: terminology, differences, and similarities. Soft Matter. 2012;8:1719–29.

    Article  CAS  Google Scholar 

  21. Lin Y-H, Tsai M-J, Fang Y-P, Fu Y-S, Huang Y-B, Wu P-C. Microemulsion formulation design and evaluation for hydrophobic compound: catechin topical application. Colloids Surf, B. 2018;161:121–8.

    Article  CAS  Google Scholar 

  22. Callender SP, Mathews JA, Kobernyk K, Wettig SD. Microemulsion utility in pharmaceuticals: implications for multi-drug delivery. Int J Pharm. 2017;526:425–42.

    Article  CAS  PubMed  Google Scholar 

  23. Bera A, Mandal A. Microemulsions: a novel approach to enhanced oil recovery: a review. Journal of Petroleum Exploration and Production Technology. 2015;5:255–68.

    Article  CAS  Google Scholar 

  24. Acharya DP, Hartley PG. Progress in microemulsion characterization. Curr Opin Colloid Interface Sci. 2012;17:274–80.

    Article  CAS  Google Scholar 

  25. Devarajan PV, Jain S. Targeted drug delivery: concepts and design. Springer 2015.

  26. Naseema A, Kovooru L, Behera AK, Kumar KP, Srivastava P. A critical review of synthesis procedures, applications and future potential of nanoemulsions. Adv Colloid Interface Sci. 2020;102318.

  27. Solans C, Solé I. Nano-emulsions: formation by low-energy methods. Curr Opin Colloid Interface Sci. 2012;17:246–54.

    Article  CAS  Google Scholar 

  28. Shah P, Bhalodia D, Shelat P. Nanoemulsion: a pharmaceutical review. Systematic Reviews in Pharmacy 1. 2010.

  29. Singh Y, Meher JG, Raval K, Khan FA, Chaurasia M, Jain NK, Chourasia MK. Nanoemulsion: concepts, development and applications in drug delivery. J Control Release. 2017;252:28–49.

    Article  CAS  PubMed  Google Scholar 

  30. Feeney OM, Crum MF, McEvoy CL, Trevaskis NL, Williams HD, Pouton CW, Charman WN, Bergström CA, Porter CJ. 50 years of oral lipid-based formulations: provenance, progress and future perspectives. Adv Drug Deliv Rev. 2016;101:167–94.

    Article  CAS  PubMed  Google Scholar 

  31. Vithani K, Jannin V, Pouton CW, Boyd BJ. Colloidal aspects of dispersion and digestion of self-dispersing lipid-based formulations for poorly water-soluble drugs. Adv Drug Deliv Rev. 2019;142:16–34.

    Article  CAS  PubMed  Google Scholar 

  32. Pouton CW, Porter CJ. Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies. Adv Drug Deliv Rev. 2008;60:625–37.

    Article  CAS  PubMed  Google Scholar 

  33. Rasoanirina BNV, Lassoued MA, Kamoun A, Bahloul B, Miladi K, Sfar S. Voriconazole-loaded self-nanoemulsifying drug delivery system (SNEDDS) to improve transcorneal permeability. Pharm Dev Technol. 2020;1–10.

  34. Batool A, Arshad R, Razzaq S, Nousheen K, Kiani MH, Shahnaz G. Formulation and evaluation of hyaluronic acid-based mucoadhesive self nanoemulsifying drug delivery system (SNEDDS) of tamoxifen for targeting breast cancer. Int J Biol Macromol. 2020.

  35. Zhao Y, Wang C, Chow AH, Ren K, Gong T, Zhang Z, Zheng Y. Self-nanoemulsifying drug delivery system (SNEDDS) for oral delivery of Zedoary essential oil: formulation and bioavailability studies. Int J Pharm. 2010;383:170–7.

    Article  CAS  PubMed  Google Scholar 

  36. Karavasili C, Andreadis II, Tsantarliotou MP, Taitzoglou IA, Chatzopoulou P, Katsantonis D, Zacharis CK, Markopoulou C, Fatouros DG. Self-nanoemulsifying drug delivery systems (SNEDDS) containing rice bran oil for enhanced fenofibrate oral delivery: in vitro digestion, ex vivo permeability, and in vivo bioavailability studies. AAPS PharmSciTech. 2020;21:1–10.

    Article  CAS  Google Scholar 

  37. Mehta S, Kaur G. Microemulsions: thermodynamic and dynamic properties. Thermodynamics. 2011;381–406.

  38. Tartaro G, Mateos H, Schirone D, Angelico R, Palazzo G. Microemulsion microstructure (s): a tutorial review. Nanomaterials. 2020;10:1657.

    Article  CAS  PubMed Central  Google Scholar 

  39. Dufrêche J-F, Zemb T. Bending: from thin interfaces to molecular films in microemulsions. Curr Opin Colloid Interface Sci. 2020.

  40. Rajpoot K, Tekade M, Pandey V, Nagaraja S, Youngren-Ortiz SR, Tekade RK. Self-microemulsifying drug-delivery system: ongoing challenges and future ahead. Drug Delivery Systems: Elsevier. 2020;393–454.

    Book  Google Scholar 

  41. Delmas T, Piraux H, Couffin A-C, Texier I, Vinet F, Poulin P, Cates ME, Bibette J. How to prepare and stabilize very small nanoemulsions. Langmuir. 2011;27:1683–92.

    Article  CAS  PubMed  Google Scholar 

  42. Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS PharmSciTech. 2010;11:314–21.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  43. Zhao L, Zhang L, Meng L, Wang J, Zhai G. Design and evaluation of a self-microemulsifying drug delivery system for apigenin. Drug Dev Ind Pharm. 2013;39:662–9.

    Article  CAS  PubMed  Google Scholar 

  44. Dholakiya A, Dudhat K, Patel J, Mori D. An integrated QbD based approach of SMEDDS and liquisolid compacts to simultaneously improve the solubility and processability of hydrochlorthiazide. J Drug Delivery Sci Technol. 2020;102162.

  45. Visetvichaporn V, Kim K-H, Jung K, Cho Y-S, Kim D-D. Formulation of self-microemulsifying drug delivery system (SMEDDS) by D-optimal mixture design to enhance the oral bioavailability of a new cathepsin K inhibitor (HL235). Int J Pharm. 2020;573:118772.

  46. Hu C-J, Zhao X-L, Li J-Z, Kang S-M, Yang C-R, Jin Y-H, Liu D, Chen D-W. Preparation and characterization of β-elemene-loaded microemulsion. Drug Dev Ind Pharm. 2011;37:765–74.

    Article  CAS  PubMed  Google Scholar 

  47. Das S, Lee SH, Chia VD, Chow PS, Macbeath C, Liu Y, Shlieout G. Development of microemulsion based topical ivermectin formulations: pre-formulation and formulation studies. Colloids Surf B Biointerfaces. 2020;189:110823.

  48. Ryu K-A, Park PJ, Kim S-B, Bin B-H, Jang D-J, Kim ST. Topical delivery of coenzyme Q10-loaded microemulsion for skin regeneration. Pharmaceutics. 2020;12:332.

    Article  CAS  PubMed Central  Google Scholar 

  49. Ciríaco SL, Carvalho IP, Neto JA, Neto JD, de Oliveira DH, Cunha AP, Cavalcante YT, da Silva DT, da Silva JA, Mineiro AL. Development of microemulsion of tamsulosin and dutasteride for benign prostatic hyperplasia therapy. Colloids Surf B Biointerfaces. 2020;185:110573.

  50. Laothaweerungsawat N, Neimkhum W, Anuchapreeda S, Sirithunyalug J, Chaiyana W. Transdermal delivery enhancement of carvacrol from Origanum vulgare L. essential oil by microemulsion. Int J Pharm. 2020;579:119052.

  51. Praça FG, Viegas JSR, Peh HY, Garbin TN, Medina WSG, Bentley MVLB. Microemulsion co-delivering vitamin A and vitamin E as a new platform for topical treatment of acute skin inflammation. Mater Sci Eng C. 2020;110:110639.

  52. Alghananim A, Özalp Y, Mesut B, Serakinci N, Özsoy Y, Güngör S. A solid ultra fine self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox for improved solubility: optimization, characterization, and in vitro cytotoxicity studies. Pharmaceuticals. 2020;13:162.

    Article  CAS  PubMed Central  Google Scholar 

  53. Kanwal T, Saifullah S, Rehman J, Kawish M, Razzak A, Maharjan R, Imran M, Ali I, Roome T, Simjee SU. Design of absorption enhancer containing self-nanoemulsifying drug delivery system (SNEDDS) for curcumin improved anti-cancer activity and oral bioavailability. J Mol Liq. 2020;114774.

  54. Qian C, McClements DJ. Formation of nanoemulsions stabilized by model food-grade emulsifiers using high-pressure homogenization: factors affecting particle size. Food Hydrocolloids. 2011;25:1000–8.

    Article  CAS  Google Scholar 

  55. Sheth T, Seshadri S, Prileszky T, Helgeson ME. Multiple nanoemulsions. Nat Rev Mater. 2020;1–15.

  56. Fatehi P, Baba AS, Misran M. Preparation and characterization of palm oil in water microemulsion for application in the food industry. Br Food J. 2020.

  57. Chen H, Khemtong C, Yang X, Chang X, Gao J. Nanonization strategies for poorly water-soluble drugs. Drug Discovery Today. 2011;16:354–60.

    Article  CAS  PubMed  Google Scholar 

  58. Rao J, McClements DJ. Formation of flavor oil microemulsions, nanoemulsions and emulsions: influence of composition and preparation method. J Agric Food Chem. 2011;59:5026–35.

    Article  CAS  PubMed  Google Scholar 

  59. Galvão K, Vicente A, Sobral PdA. Development, characterization, and stability of O/W pepper nanoemulsions produced by high-pressure homogenization. Food Bioproc Tech. 2018;11:355–367.

  60. Juttulapa M, Piriyaprasarth S, Takeuchi H, Sriamornsak P. Effect of high-pressure homogenization on stability of emulsions containing zein and pectin. Asian J Pharm Sci. 2017;12:21–7.

    Article  PubMed  Google Scholar 

  61. Yadav KS, Kale K. High pressure homogenizer in pharmaceuticals: understanding its critical processing parameters and applications. J Pharm Innov. 2019;1–12.

  62. Ahmad N, Ahmad R, Al-Qudaihi A, Alaseel SE, Fita IZ, Khalid MS, Pottoo FH. Preparation of a novel curcumin nanoemulsion by ultrasonication and its comparative effects in wound healing and the treatment of inflammation. RSC Adv. 2019;9:20192–206.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  63. Zeng Z, Zhou G, Wang X, Huang EZ, Zhan X, Liu J, Wang S, Wang A, Li H, Pei X. Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion. Int J Nanomed. 2010;5:567.

    Article  CAS  Google Scholar 

  64. Sugumar S, Singh S, Mukherjee A, Chandrasekaran N. Nanoemulsion of orange oil with non ionic surfactant produced emulsion using ultrasonication technique: evaluating against food spoilage yeast, Applied. Nanoscience. 2016;6:113–20.

    Article  CAS  Google Scholar 

  65. Azizi M, Esmaeili F, Partoazar A, Ejtemaei Mehr S, Amani A. Efficacy of nano-and microemulsion-based topical gels in delivery of ibuprofen: an in vivo study. J Microencapsul. 2017;34:195–202.

  66. Akbas E, Soyler B, Oztop MH. Formation of capsaicin loaded nanoemulsions with high pressure homogenization and ultrasonication. Lwt. 2018;96:266–73.

    Article  CAS  Google Scholar 

  67. Li Y, Zhao X, Zu Y, Zhang Y. Preparation and characterization of paclitaxel nanosuspension using novel emulsification method by combining high speed homogenizer and high pressure homogenization. Int J Pharm. 2015;490:324–33.

    Article  CAS  PubMed  Google Scholar 

  68. Cho YH, Kim S, Bae EK, Mok C, Park J. Formulation of a cosurfactant-free o/w microemulsion using nonionic surfactant mixtures. J Food Sci. 2008;73:E115–21.

    Article  CAS  PubMed  Google Scholar 

  69. van der Schaaf US, Karbstein HP. Fabrication of nanoemulsions by rotor-stator emulsification. Nanoemulsions: Elsevier; 2018. p. 141–74.

    Google Scholar 

  70. Mohammed AN, Ishwarya SP, Nisha P. Nanoemulsion versus microemulsion systems for the encapsulation of beetroot extract: comparison of physicochemical characteristics and betalain stability. Food Bioprocess Technol. 2021;14:133–50.

    Article  CAS  Google Scholar 

  71. Scholz P, Keck CM. Nanoemulsions produced by rotor–stator high speed stirring. Int J Pharm. 2015;482:110–7.

    Article  CAS  PubMed  Google Scholar 

  72. Santos García J, Calero Romero N, Trujillo Cayado LA, Martín Piñero MJ, Muñoz García J. Processing and formulation optimization of mandarin essential oil-loaded emulsions developed by microfluidization. Materials. 2020;13(16):3486.

  73. Bahuguna A, Ramalingam S, Kim M. Formulation, characterization, and potential application of nanoemulsions in food and medicine. Nanotechnology for Food, Agriculture, and Environment. Springer 2020;39–61.

  74. Kulkarni CV. Lipid self-assemblies and nanostructured emulsions for cosmetic formulations. Cosmetics. 2016;3:37.

    Article  CAS  Google Scholar 

  75. Ren G, Sun Z, Wang Z, Zheng X, Xu Z, Sun D. Nanoemulsion formation by the phase inversion temperature method using polyoxypropylene surfactants. J Colloid Interface Sci. 2019;540:177–84.

    Article  CAS  PubMed  Google Scholar 

  76. Feng J, Rodríguez‐Abreu C, Esquena J, Solans C. A concise review on nano-emulsion formation by the phase inversion composition (PIC) method. J Surfactants Deterg. 2020.

  77. Kotta S, Khan AW, Ansari S, Sharma R, Ali J. Formulation of nanoemulsion: a comparison between phase inversion composition method and high-pressure homogenization method. Drug Delivery. 2015;22:455–66.

    Article  CAS  PubMed  Google Scholar 

  78. Maestro A, Solè I, González C, Solans C, Gutiérrez JM. Influence of the phase behavior on the properties of ionic nanoemulsions prepared by the phase inversion composition method. J Colloid Interface Sci. 2008;327:433–9.

    Article  CAS  PubMed  Google Scholar 

  79. Parmar PK, Rao SG, Bansal AK. Co-processing of small molecule excipients with polymers to improve functionality. Expert Opin Drug Deliv. 2021.

  80. Dhaval M, Devani J, Parmar R, Soniwala M, Chavda J. Formulation and optimization of microemulsion based sparfloxacin in-situ gel for ocular delivery: In vitro and ex vivo characterization. J Drug Delivery Sci Technol. 2020;55:101373.

  81. Hashem FM, Shaker DS, Ghorab MK, Nasr M, Ismail A. Formulation, characterization, and clinical evaluation of microemulsion containing clotrimazole for topical delivery. AAPS PharmSciTech. 2011;12:879–86.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  82. Shinde UA, Modani SH, Singh KH. Design and development of repaglinide microemulsion gel for transdermal delivery. AAPS PharmSciTech. 2018;19:315–25.

    Article  CAS  PubMed  Google Scholar 

  83. Tiwari N, Sivakumar A, Mukherjee A, Chandrasekaran N. Enhanced antifungal activity of Ketoconazole using rose oil based novel microemulsion formulation. Journal of Drug Delivery Science and Technology. 2018;47:434–44.

    Article  CAS  Google Scholar 

  84. Dhaval M, Panjwani M, Parmar R, Soniwala M, Dudhat K, Chavda J. Application of simple lattice design and desirability function for formulating and optimizing SMEDDS of clofazimine. J Pharm Innov. 2020;1–12.

  85. Prajapati HN, Dalrymple DM, Serajuddin AT. A comparative evaluation of mono-, di-and triglyceride of medium chain fatty acids by lipid/surfactant/water phase diagram, solubility determination and dispersion testing for application in pharmaceutical dosage form development. Pharm Res. 2012;29:285–305.

    Article  CAS  PubMed  Google Scholar 

  86. Patel V, Lalani R, Bardoliwala D, Ghosh S, Misra A. Lipid-based oral formulation strategies for lipophilic drugs. AAPS PharmSciTech. 2018;19:3609–30.

    Article  CAS  PubMed  Google Scholar 

  87. Kalepu S, Manthina M, Padavala V. Oral lipid-based drug delivery systems—an overview. Acta Pharmaceutica Sinica B. 2013;3:361–72.

    Article  Google Scholar 

  88. Stuchlík M, Zak S. Lipid-based vehicle for oral drug delivery. Biomedical Papers-Palacky University in Olomouc. 2001;145:17–26.

    Article  Google Scholar 

  89. Khan AW, Kotta S, Ansari SH, Sharma RK, Ali J. Potentials and challenges in self-nanoemulsifying drug delivery systems. Expert Opin Drug Deliv. 2012;9:1305–17.

    Article  CAS  PubMed  Google Scholar 

  90. Stella VJ. Chemical drug stability in lipids, modified lipids, and polyethylene oxide-containing formulations. Pharm Res. 2013;30:3018–28.

    Article  CAS  PubMed  Google Scholar 

  91. Gibson L. Lipid-based excipients for oral drug delivery. Drugs and the Pharmaceutical sciences. 2007;170:33.

    CAS  Google Scholar 

  92. Singh B, Beg S, Khurana RK, Sandhu PS, Kaur R, Katare OP. Recent advances in self-emulsifying drug delivery systems (SEDDS). Critical Reviews™ in Therapeutic Drug Carrier Systems. 2014:31.

  93. Pandey V, Kohli S. Lipids and surfactants: The inside story of lipid-based drug delivery systems. Critical Reviews™ in Therapeutic Drug Carrier Systems. 2018:35.

  94. Kuentz M. Lipid-based formulations for oral delivery of lipophilic drugs. Drug Discov Today Technol. 2012;9:e97–104.

    Article  CAS  Google Scholar 

  95. Rani S, Rana R, Saraogi GK, Kumar V, Gupta U. Self-emulsifying oral lipid drug delivery systems: advances and challenges. AAPS PharmSciTech. 2019;20:129.

    Article  CAS  PubMed  Google Scholar 

  96. Casiraghi A, Selmin F, Minghetti P, Cilurzo F, Montanari L. Nonionic surfactants: polyethylene glycol (PEG) ethers and fatty acid esters as penetration enhancers. Percutaneous Penetration Enhancers Chemical Methods in Penetration Enhancement. Springer 2015;251–271.

  97. Cannon JB, Long MA. 11 emulsions, microemulsions, and lipid-based drug delivery systems for drug solubilization and delivery—Part II: oral applications. Water-Insoluble Drug Formulation. 2018.

  98. Zheng Y, Zheng M, Ma Z, Xin B, Guo R, Xu X. 8 - Sugar fatty acid esters, in: M.U. Ahmad, X. Xu (Eds.). Polar Lipids. Elsevier 2015;215–243.

  99. Aman ZM, Olcott K, Pfeiffer K, Sloan ED, Sum AK, Koh CA. Surfactant adsorption and interfacial tension investigations on cyclopentane hydrate. Langmuir. 2013;29:2676–82.

    Article  CAS  PubMed  Google Scholar 

  100. Attwood D, Florence AT. FASTtrack Physical Pharmacy. Pharmaceutical Press. 2012.

  101. Kale SN, Deore SL. Emulsion micro emulsion and nano emulsion: a review. Systematic Reviews in Pharmacy. 2017;8:39.

    Article  CAS  Google Scholar 

  102. The organic chemistry of surfactants. Surf Sci Technol. 2005;29–79.

  103. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’drug delivery systems. Eur J Pharm Sci. 2000;11:S93–8.

    Article  CAS  PubMed  Google Scholar 

  104. Ahmed N, Kermanshahi B, Ghazani SM, Tait K, Tcheng M, Roma A, Callender SP, Smith RW, Tam W, Wettig SD. Avocado-derived polyols for use as novel co-surfactants in low energy self-emulsifying microemulsions. Sci Rep. 2020;10:1–14.

    Article  CAS  Google Scholar 

  105. McClements DJ, Jafari SM. Improving emulsion formation, stability and performance using mixed emulsifiers: a review. Adv Coll Interface Sci. 2018;251:55–79.

    Article  CAS  Google Scholar 

  106. Szumała P. Structure of microemulsion formulated with monoacylglycerols in the presence of polyols and ethanol. J Surfactants Deterg. 2015;18:97–106.

    Article  PubMed  CAS  Google Scholar 

  107. Nan Y, Li W, Jin Z. Role of alcohol as a cosurfactant at the brine–oil interface under a typical reservoir condition. Langmuir. 2020;36:5198–207.

    Article  CAS  PubMed  Google Scholar 

  108. Man N, Wang Q, Li H, Adu-Frimpong M, Sun C, Zhang K, Yang Q, Wei Q, Ji H, Toreniyazov E. Improved oral bioavailability of myricitrin by liquid self-microemulsifying drug delivery systems. Journal of Drug Delivery Science and Technology. 2019;52:597–606.

    Article  CAS  Google Scholar 

  109. Chung C, McClements DJ. Characterization of physicochemical properties of nanoemulsions: appearance, stability, and rheology. Nanoemulsions: Elsevier; 2018. p. 547–76.

    Google Scholar 

  110. Jagdale SC, Deore GK, Chabukswar AR. Development of microemulsion based nabumetone transdermal delivery for treatment of arthritis. Recent Pat Drug Delivery Formulation. 2018;12:130–49.

    Article  CAS  Google Scholar 

  111. Ramasahayam B, Eedara BB, Kandadi P, Jukanti R, Bandari S. Development of isradipine loaded self-nano emulsifying powders for improved oral delivery: in vitro and in vivo evaluation. Drug Dev Ind Pharm. 2015;41:753–63.

    Article  CAS  PubMed  Google Scholar 

  112. Cherniakov I, Domb AJ, Hoffman A. Self-nano-emulsifying drug delivery systems: an update of the biopharmaceutical aspects. Expert Opin Drug Deliv. 2015;12:1121–33.

    Article  CAS  PubMed  Google Scholar 

  113. Kadu PJ, Kushare SS, Thacker DD, Gattani SG. Enhancement of oral bioavailability of atorvastatin calcium by self-emulsifying drug delivery systems (SEDDS). Pharm Dev Technol. 2011;16:65–74.

    Article  CAS  PubMed  Google Scholar 

  114. Poomanee W, Chaiyana W, Wickett RR, Leelapornpisid P. Stability and solubility improvement of Sompoi (Acacia concinna Linn.) pod extract by topical microemulsion. Asian J Pharm Sci. 2017;12:386–393.

  115. Pandey SS, Maulvi FA, Patel PS, Shukla MR, Shah KM, Gupta AR, Joshi SV, Shah DO. Cyclosporine laden tailored microemulsion-gel depot for effective treatment of psoriasis: In vitro and in vivo studies. Colloids Surf B Biointerfaces. 2020;186:110681.

  116. Porter CJ, Trevaskis NL, Charman WN. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discovery. 2007;6:231–48.

    Article  CAS  PubMed  Google Scholar 

  117. Porter CJ, Charman WN. Lipid-based formulations for oral administration: opportunities for bioavailability enhancement and lipoprotein targeting of lipophilic drugs. J Recept Signal Transduction. 2001;21:215–57.

    Article  CAS  Google Scholar 

  118. Nazzal S, Wang Y. Characterization of soft gelatin capsules by thermal analysis. 2001;230:35–45.

  119. Chang RK, Raghavan KS, Hussain MA. A study on gelatin capsule brittleness: moisture tranfer between the capsule shell and its content. 1998;87:556–558.

  120. Oh DH, Kang JH, Kim DW, Lee BJ, Kim JO, Yong CS, Choi HG. Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier. 2011;420:412–418.

  121. Čerpnjak K, Zvonar A, Vrečer F, Gašperlin M. Development of a solid self-microemulsifying drug delivery system (SMEDDS) for solubility enhancement of naproxen. 2015;41:1548–1557.

  122. Bhagwat Durgacharan V, D’Souza John I. Development of solid self micro emulsifying drug delivery system with neusilin US2 for enhanced dissolution rate of telmisartan. 2012;4:398–407.

  123. Deshmukh A, Kulkarni S. Solid self-microemulsifying drug delivery system of ritonavir. 2014;40:477–487.

  124. Dangre PV, Gilhotra RM, Dhole SN. Formulation and development of solid self micro-emulsifying drug delivery system (S-SMEDDS) containing chlorthalidone for improvement of dissolution. 2016;46:633–644.

  125. Li L, Yi T, Lam CW. Effects of spray-drying and choice of solid carriers on concentrations of Labrasol® and Transcutol® in solid self-microemulsifying drug delivery systems (SMEDDS). 2013;18:545–560.

  126. Jaiswal P, Aggarwal G, Harikumar SL, Singh K. Development of self-microemulsifying drug delivery system and solid-self-microemulsifying drug delivery system of telmisartan. 2014;4:195.

  127. Taylor LS, Zhang GG. Physical chemistry of supersaturated solutions and implications for oral absorption. 2016;101:122–142.

  128. Craig DQ. The mechanisms of drug release from solid dispersions in water-soluble polymers. 2002;231:131–144.

  129. Buckley ST, Frank KJ, Fricker G, Brandl M. Biopharmaceutical classification of poorly soluble drugs with respect to “enabling formulations,”. 2013;50:8–16.

  130. Schittny A, Huwyler J, Puchkov M. Mechanisms of increased bioavailability through amorphous solid dispersions: a review. 2020;27:110–127.

  131. Shah N, Sandhu H, Choi DS, Chokshi H, Malick AW. S. Technology, Amorphous solid dispersions. 2014.

  132. Dokania S, Joshi AK. Self-microemulsifying drug delivery system (SMEDDS)–challenges and road ahead. 2015;22:675–690.

  133. Xu S, Dai WG. Drug precipitation inhibitors in supersaturable formulations. 2013;453:36–43.

  134. Bevernage J, Brouwers J, Brewster ME, Augustijns P. Evaluation of gastrointestinal drug supersaturation and precipitation: strategies and issues. 2013;453:25–35.

  135. Mukherjee T, Plakogiannis FM. Pharmacology, Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole. 2010;62:1112–1120.

  136. Gao P,  Morozowich W. Development of supersaturatable self-emulsifying drug delivery system formulations for improving the oral absorption of poorly soluble drugs. 2006;3:97–110.

  137. Jo K, Kim H, Khadka P, Jang T, Kim SJ, Hwang SH, Lee J. Enhanced intestinal lymphatic absorption of saquinavir through supersaturated self-microemulsifying drug delivery systems. 2020;15:336–346.

  138. Bennett-Lenane H, O’Shea JP, O’Driscoll CM, Griffin BT. A retrospective biopharmaceutical analysis of> 800 approved oral drug products: are drug properties of solid dispersions and lipid-based formulations distinctive?. 2020.

  139. Strickley RG. Currently marketed oral lipid-based dosage forms: drug products and excipients. Drugs and the Pharmaceutical sciences. 2007;170:1.

    CAS  Google Scholar 

  140. Shrestha S, Bala R, Arora S. Lipid-based drug delivery systems, J Pharm. 2014.

  141. Kohli K, Chopra S, Dhar D, Arora S, Khar RK. Self-emulsifying drug delivery systems: an approach to enhance oral bioavailability. Drug Discovery Today. 2010;15:958–65.

    Article  CAS  PubMed  Google Scholar 

  142. Rane SS, Anderson BD. What determines drug solubility in lipid vehicles: is it predictable?. 2008;60:638–656.

Download references

Author information

Authors and Affiliations

  1. B.K. Mody Government Pharmacy College, Polytechnic Campus, Near Ajidam, Rajkot, Gujarat, India

    Mori Dhaval, Poonam Vaghela, Kajal Patel, Keshvi Sojitra, Mohini Patel, Sushma Patel, Sunny Shah, Ravi Manek & Ramesh Parmar

  2. K. V. Virani Institute of Pharmacy and Research Centre, Badhada, Gujarat, India

    Kiran Dudhat

Authors
  1. Mori Dhaval
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Poonam Vaghela
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Kajal Patel
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Keshvi Sojitra
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Mohini Patel
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. Sushma Patel
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. Kiran Dudhat
    View author publications

    You can also search for this author in PubMed Google Scholar

  8. Sunny Shah
    View author publications

    You can also search for this author in PubMed Google Scholar

  9. Ravi Manek
    View author publications

    You can also search for this author in PubMed Google Scholar

  10. Ramesh Parmar
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Mori Dhaval.

Ethics declarations

Conflict of interests

The authors declare no competing interests.

Additional information

Publisher's Note

Springer Nature remains neutral with regard to jurisdictional claims in published maps and institutional affiliations.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Dhaval, M., Vaghela, P., Patel, K. et al. Lipid-based emulsion drug delivery systems — a comprehensive review. Drug Deliv. and Transl. Res. 12, 1616–1639 (2022). https://doi.org/10.1007/s13346-021-01071-9

Download citation

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s13346-021-01071-9

Keywords

Search

Navigation