In recent years, there has been increasing interest in the use of formulations containing lipid-based excipients that comprise combinations of synthetic or semisynthetic lipids with surfactants, co-surfactants or co-solvents. This review is generally focussed on lipid-based excipients in pharmaceutical formulations which improves the oral bioavailability of poorly water-soluble drugs. Lipid-based formulations can reduce the limitations of slow and incomplete dissolution of poorly water-soluble drugs, and facilitate the formation of solubilised phases from which absorption may occur. The improvement of bio-availability of drugs is one of the greatest challenges in drug formulations. This review discusses novel lipids like Compritol 888 ATO, Dynasan 114, Glyceryl monooleate (GMO), Maisine CC and Precirol ATO 5 focussing on how these can be employed for devising efficient drug delivery systems and also the in vivo effect and fate of lipid excipients.
Cite this article:
Soma Santra, Sutapa Biswas Majee. Lipid based Vehicles and Lipid-based Excipients in Drug delivery. Research Journal of Pharmacy and Technology. 2022; 15(5):2334-8. doi: 10.52711/0974-360X.2022.00388
Soma Santra, Sutapa Biswas Majee. Lipid based Vehicles and Lipid-based Excipients in Drug delivery. Research Journal of Pharmacy and Technology. 2022; 15(5):2334-8. doi: 10.52711/0974-360X.2022.00388 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2022-15-5-70
1. Haywood A and Glass BD. Pharmaceutical excipients – where do we begin?. Australian Prescriber. 2011; 34(4): 112-114.
2. Katdare A and Chaubal MV. Excipient development for pharmaceutical, biotechnology, and drug delivery systems. Informa Health Care, New York. 2006.
3. Somnache SN, Godbole AM and Gajare PS, Kashyap S. Significance of pharmaceutical excipients on solid dosage form development: A brief review. Asian Journal of Pharmaceutical Research. 2016; 6(3): 193-202.
4. Pifferi G and Restani P. The safety of pharmaceutical excipients. Il Farmaco. 2003; 58(8): 541-550.
5. Raval AJ and Patel MM. Techniques to improve bioavailability of poorly water-soluble drugs – A review. Research Journal of Pharmaceutical Dosage Forms and Tech. 2011; 3(5): 182-192.
6. Potphode VR, Deshmukh AS and Mahajan VR. Self-micro emulsifying drug delivery system: An approach for enhancement of bioavailability of poorly water-soluble drugs. Asian Journal of Pharmaceutical Technology. 2016; 6 (3): 159-168.
7. Saxena S, et al. Lipid Excipients in Self Emulsifying Drug Delivery Systems. Asian Journal of Biomedical and Pharmaceutical Sciences. 2013; 3(22): 16-22.
8. Bhore SD. A review on solid dispersion as a technique for enhancement of bioavailability of poorly water-soluble drugs. Research Journal of Pharmaceutical Technology. 2014; 7(12): 1485-1491.
9. Bhairav BA, Bachhav JK and Saudagar RB. Review on Solubility Enhancement Techniques. Asian J. Pharm. Res. 2016; 6(3): 147-152.
10. Giri TK, Mishra S and Tripathi DK. Carriers used for the development of solid dispersion for poorly water-soluble drugs. Research Journal of Pharmaceutical Technology. 2011; 4(3): 356-366.
11. Pouton CW and Porter CJH. Formulation of lipid-based delivery system for oral administration: Materials, methods and strategies. Advanced Drug Delivery Reviews. 2007; 60: 625-637.
12. Vakhariya RR, Talokar SS, Salunkhe VR and Magdum CS. Formulation development and optimization of simvastatin loaded solid lipid nanoparticles. Asian Journal of Research in Pharmaceutical Sciences 2017; 7(1): 49-52.
13. Sanghavi S, Polara M, Patel D, et al. Nanoparticle drug delivery to brain – A Review. Research Journal of Pharmaceutical Technology. 2012; 5(1): 8-13.
14. Sharma A, Dubey A and Yadav R. Solid lipid nanoparticles: A promising nanotechnology. Research Journal of Pharmaceutical Dosage Forms and Tech. 2011; 3(5): 167-175.
15. Kalepu S, Manthina M and Padavala V. Oral lipid drug delivery system- an overview. Acta Pharmaceutica Sinica B. 2013; 3(6): 361-372.
16. Devi R and Agarwal S. Some multifunctional lipid excipients and their pharmaceutical applications. International Journal of Pharmacy and Pharmaceutical Sciences. 2019; 11(9): 1-17.
17. Rajput DS et al. Novel integrated approach for the strategic delivery of hydrophobic drugs by the use of self-emulsifying drug delivery system. Journal of Applied Sciences. 2012; 12(6): 502-517.
18. Cao Y, Marra M and Anderson BD. Predictive relationships for the effects of triglycerides ester concentration and water uptake on solubility and partitioning of small molecules into lipid vehicles. Journal of Pharmaceutical Sciences. 2004; 93(11): 2768-2779.
19. Collnot EM, et al. Influence of vitamin E TPGS poly (ethylene glycol) chain length on apical efflux transporters in Caco-2 cell monolayers. Journal of Controlled Release. 2006; 111: 35-40.
20. Strickley RG. Currently marketed oral lipid-based dosage form: drugs, products and excipients. In Oral lipid formulations: enhancing the bioavailability of poorly water-soluble drugs, Edited by Hauss DJ. Informa Healthcare, New York. 2007; 1-31.
21. Hu LD, et al. Preparation and enhanced oral bioavailability of cryptotanshinone loaded solid lipid nanoparticles. AAPS Advances in the Pharmaceutical Sciences. 2010; 11(2): 582-587.
22. Patere SN, et al. Compritol 888 ATO a lipid excipient for sustained release of highly water soluble active: formulation, scale-up and IVIVC study. Current Drug Delivery. 2013; 10(5): 548-556.
23. Aburahma MH and Badr-Eldin M. Compritol 888 ATO: A multifunctional lipid excipient in drug delivery systems and nano pharmaceuticals. Expert Opinion Drug Delivery. 2014; 11(12): 1865-1883.
24. Cavallari C, Fini A and Ospitali F. Mucoadhesive multiparticulate patch for intrabuccal controlled delivery of lidocaine. European Journal of Pharmaceutics and Biopharmaceutics. 2013; 83: 405-414.
25. Wei L, et al. Preparation and characterization of loperamide loaded dynasan 114 solid lipid nanoparticles for increased oral absorption in the treatment of diarrhea. Frontiers in Pharmacology. 2016; 7(332): 1-9.
26. Bertoni S, et al. Glutathione-loaded solid lipid nanoparticles as innovative delivery system for oral antioxidant therapy. Pharmaceutics. 2019; 11(364): 1-17.
27. Lai J, et al. Glyceryl monooleate/poloxamer 407 cubic nanoparticles as oral drug delivery systems: I. In vitro evaluation and enhanced oral bioavailability of the poorly water-soluble drug Simvastatin. American Association of Pharmaceutical Scientists. 2009; 10(3): 960-966.
28. Lim DG and Jeong SH. Effect of the glyceryl monooleate-based lyotropic phases on skin permeation using in vitro diffusion and skin imaging. Asian Journal of Pharmaceutical Sciences. 2014; 9(6): 324-329.
29. Steluti R, et al. Topical glycerol monooleate/propylene glycol formulations enhance 5-aminolevulinic acid in vitro skin delivery and in vivo protophorphyrin IX accumulation in hairless mouse skin. European Journal of Pharmaceutics and Biopharmaceutics. 2005; 60: 439-444.
30. Nasr AM, Qushawy MK and Swidan SA. Quality by design for the development and analysis of enhanced in-situ forming vesicles for the improvement of the bioavailability of fexofenadine HCl in vitro an in vivo. Pharmaceutics. 2020; 12(409): 1-22.
31. Salunkhe SS, Bhatia NM and Bhatia MS. Implication of formulation design on lipid-based nanostructured carrier system for drug delivery to brain. Drug Delivery, Early Online. 2014; 1-11.
32. Ashok P, Meyyanathan SN and Vadivelan R. Nanosuspensions by solid lipid nanoparticles method for the formulation and in vitro/in vivo characterization of nifedipine. Asian Journal of Research in Pharmaceutical Sciences. 2021; 11(1): 1-6.
33. Farvin KHS and Jacobsen C. Potato peel extract as a natural antioxidant in chilled storage of minced horse mackerel (Trachurus trachurus): Effect on lipid and protein oxidation. Food Chemistry. 2012; 131: 843-851.
34. Nanjwade BK, et al. Functions of lipids for enhancement of oral bioavailability of poorly water-soluble drugs. Scientia Pharmaceutica. 2011; 79: 705-727.
35. Sitrin MD. Digestion and absorption of dietary triglycerides. In the Gastrointestinal System: Gastrointestinal, Nutritional and Hepatobiliary Physiology. Edited by Leung PS. 2014; 159-178.
36. Muller RH, Ruhl D and Runge SA. Biodegradation of solid lipid nanoparticles as a function of lipase incubation time. International Journal of Pharmaceutics. 1996; 144: 115-121.
37. Harde H, Das M and Jain S. Solid lipid nanoparticles: an oral bioavailability enhancer vehicle. Expert Opinion Drug Delivery. 2011; 8(11): 1407-1424.