Liposomal Formulations for Improved Bioavailability of Poorly Soluble Drugs
Abstract
Many medicines in clinical use or in development are water-insoluble and have low bioavailability (BA). Because of its biocompatibility and capacity to encapsulate hydrophobic compounds in the lipid domain, the liposomal delivery method has gained attention as one of the most notable techniques to increasing dissolution and, ultimately, absorption in the gastrointestinal (GI) tract. Due to its relatively large size, there have been various problems, including structural instability in the GI tract and low permeability across intestinal epithelia. Furthermore, despite the success of parenteral liposomes, no liposomal formulations for oral use have been approved thus far. Liposomal oral administration has resurged since the number of published studies has increased dramatically over the previous decade.
References
2. Da Silva FL, Marques MB, Kato KC, et al. Nanonization techniques to overcome poor water-solubility with drugs. Expert Opin Drug Discov. 2020;15(7):853–864.
3. Amidon, G.L.; Lennernäs, H.; Shah, V.P.; Crison, J.R. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res 1995, 12, 413–420.
4. Williams, H.D.; Trevaskis, N.L.; Charman, S.A.; Shanker, R.M.; Charman, W.N.; Pouton, C.W.; Porter, C.J. Strategies to address low drug solubility in discovery and development. Pharmacol. Rev. 2013, 65, 315–499.
5. Krishnaiah, Y.S. Pharmaceutical technologies for enhancing oral bioavailability of poorly soluble drugs. J. Bioequiv. Available. 2010, 2, 28–36.
6. Van, HP, Rogue, V, Brumec, M. Instant solubilization of poorly water-soluble drugs by in-situ loading of aqueous phospholipid dispersions suitable for parenteral administration. PDA J. Pharm. Sci. Technol.
7. Shen, Y, Tu, J. Preparation and Ocular Pharmacokinetics of Ganciclovir Liposomes. AAPS Journal. 2007; 9(3):E371- E377. Bioavailability, solubility, liposome, nano sponges.
8. E. Nelson, E. L. Knoechel, W. E. Hamlin, J. G. Wagner, Influence of the absorption rate of tolbutamide on the rate of decline of blood sugar levels in normal humans. Int J Pharm. 51, 1962, 509-514.
9. S. L Lin, L. Lachman, C. J. Swartz, C. F. Heubner, Preformulation investigation 1. Relation of salt forms and biological activity of an experimental antihypertensive. J. Pharm.Sci., 61(9), 1972, 1418-1422.
10. A.Arien, C. Goigoux, C. Baquey, B. Dupuy, Study of in vitro and in vivo stability of liposomes loaded with calcitonin or indium in the gastrointestinal tract. Life Sci. 53, 1279–1290, 1993.
11. Arien, N. Henry-Toulmé, B. Dupuy, Calcitonin-loaded liposomes: stability under acidic conditions and bile salts-induced disruption resulting in calcitonin–phospholipid complex formation. Biochim. Biophys. Acta 1193, 1994, 93–100.
12. Abu Lila, A.S.; Ishida, T. Liposomal Delivery Systems: Design Optimization and Current Applications. Biol. Pharm. Bull. 2017, 40, 1–10.
13. Shen, Y, Tu, J. Preparation and Ocular Pharmacokinetics of Ganciclovir Liposomes. AAPS Journal. 2007; 9(3):E371-E377
14. hossan. M. Hossann, T. Wang, Z. Syunyaeva et al. Non-ionic Gd-based MRI contrast agents are optimal for encapsulation into phosphatidyldiglycerol-based thermosensitive liposomes. J Control Release. 166, 2013, 22– 29
15. Chen, D.; Xia, D.; Li, X.; Zhu, Q.; Yu, H.; Zhu, C.; Gan, Y. Comparative Study of Pluronic((R)) F127-Modified Liposomes and Chitosan-Modified Liposomes for Mucus Penetration and Oral Absorption of Cyclosporine A in Rats. Int. J. Pharm.2013, 449, 1–9.
16. Ting, J.M.; Porter III, W.W.; Mecca, J.M.; Bates, F.S.; Reineke, T.M. Advances in polymer design for enhancing oral drug solubility and delivery. Bioconjug. Chem. 2018, 29, 939–952
17. Maheshkumar SS, Reddy KN, Goud PP, Kiranmayi N, Arvind G. Formulation and Characterization of Doxorubicin Hydrochloride Liposomes by Double Emulsion Method. Int Res J Pharm 2013;4(4):197-201.
18. Fong, S.Y.; Brandl, M.; Bauer-Brandl, A. Phospholipid-Based Solid Drug Formulations for Oral Bioavailability Enhancement: A Meta-Analysis. Eur. J. Pharm. Sci. 2015, 80, 89–110.