Formulation And Evaluation of Oral Micelles Carriers for Solubility Enhancement
Keywords:
Bioavailability, Lovastatin, Dissolution, Solvent evaporation methodAbstract
In the present study, oral micelles with a hydrophilic polymer and surfactant were developed using the hot homogenization technique process to improve the dissolution. The physicochemical properties of the lovastatin containing oral micelles were characterized using scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction, and a particle-size analyzer. The mean particle size of all Oral Micelles that were prepared was less than 500 nm. Polyethylene glycol (PEG) oral micelles significantly increased the maximum dissolution when compared with propylene glycol (PG), and polyvinylpyrrolidone (PVP) oral micelles. In this study, the oral micelles with a LO:PC:LC; 2:1:1.5 have rapid dissolution within 30 minutes, in addition to good oral bioavailability, with These results suggest that the preparation of lovastatin oral micelles using the hot homogenization process is a promising approach to improve the dissolution and absorption properties of drug.
Downloads
Metrics
References
Choi M., Maibach H. Liposomes and niosomes as topical drug delivery systems. Skin Pharmacol. Physiol. 2005; 18:209–219.
Dinh H.T.T., Tran P.H.L., Duan W., Lee B.-J., Tran T.T.D. Nano-sized solid dispersions based on hydrophobic-hydrophilic conjugates for dissolution enhancement of poorly water-soluble drugs. Int. J. Pharm. 2017; 533:93–98.
Jang K, Yoon S, Kim SE, et al. Novel nanocrystal formulation of megestrol acetate has improved bioavailability compared with the conventional micronized formulation in the fasting state. Drug Des Devel Ther. 2014; 8:851–858.
Montenegro L., Sinico C., Castangia I., Carbone C., Puglisi G. Idebenone-loaded oral micelles for drug delivery to the skin: in vitro evaluation. Int. J. Pharm. 2012; 434:169–174.
Müller R.H., Radtke M., Wissing S.A. Oral micelles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv. Drug Deliv. Rev. 2002;54: S131– S155.
Shekunov BY, Chattopadhyay P, Seitzinger J, Huff R. Nanoparticles of poorly water-soluble drugs prepared by supercritical fluid extraction of emulsions. Pharm Res. 2006;23(1):196–204.
Wissing S.A., Müller R.H. The influence of oral micelleson skin hydration and viscoelasticity– in vivo study. Eur. J. Pharm. Biopharm. 2003; 56:67–72.
Yallapu M.M., Jaggi M., Chauhan S.C. β-Cyclodextrin-curcumin self-assembly enhances curcumin delivery in prostate cancer cells. Colloids Surf. B: Biointerfaces. 2010; 79:113–125.
Zhang ZB, Shen ZG, Wang JX, Zhao H, Chen JF, Yun J. Nanonization of megestrol acetate by liquid precipitation. Ind Eng Chem Res. 2009; 48(18):8493–8499.
Kim MS, Kim JS, Cho W, et al. Supersaturatable formulations for the enhanced oral absorption of sirolimus. Int J Pharm. 2013;445(1–2): 108–116.
Da Silva Júnior W.F., De Oliveira Pinheiro J.G., Moreira C.D., de Souza F.J.J., de Lima Á.A.N. Multifunctional Systems for Combined Delivery, Biosensing and Diagnostics. Elsevier; Amsterdam, The Netherlands: 2017. Alternative technologies to improve solubility and stability of poorly water-soluble drugs; pp. 281–305.
Jang D.-J., Sim T., Oh E. Formulation and optimization of spray-dried amlodipine solid dispersion for enhanced oral absorption. Drug Dev. Ind. Pharm. 2013; 39:1133–1141.
Cocero MJ, Martín A, Mattea F, Varona S. Encapsulation and co- precipitation processes with supercritical fluids: fundamentals and applications. J Supercrit Fluids. 2009;47(3):546–555.
Yin X, Daintree LS, Ding S, et al. Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs. Drug Des Devel Ther. 2015;9: 2801–2810.
Kapadia R., Jain M, Patel D., Devkar R, Sawant K.. Nano-emulsomes for Back of the Eye Delivery of Ganciclovir: Formulation Optimization, Characterization & In vitro/In vivo Evaluation. Pharmaceutical development and technology. 2023, 28. 1-39.
Kim MS, Kim JS, Park HJ, Cho WK, Cha KH, Hwang SJ. Enhanced bio- availability of sirolimus via preparation of solid dispersion nanoparticles using a supercritical antisolvent process. Int J Nanomedicine. 2011;6: 2997–3009.
Lee DH, Yeom DW, Song YS, et al. Improved oral absorption of dutasteride via Soluplus®- based supersaturable self-emulsifying drug delivery system (S-SEDDS). Int J Pharm. 2014;478(1):341–347.
Junghanns JU, Müller RH. Nanocrystal technology, drug delivery and clinical applications. Int J Nanomedicine. 2008;3(3):295–310.
Kapadia R, Jain M, Patel D, Devkar R, Sawant K, Amelioration of carbon tetrachloride induced hepatotoxicity in rats by standardized Feronia limonia. Linn leaf extracts
Kapadia R, Shevalkar G, Das U, Singhai V, Bari D, Pardeshi CV. Introduction to Quality by Design. In: Jain, N.K., Bajwa, N. (eds) Introduction to Quality by Design (QbD). Springer, Singapore, 2024.
Kamani P, Parikh K, Kapadia R, Sawant K, Phospholipid based ultra-deformable nanovesicular gel for transcutaneous application: QbD based optimization, characterization and pharmacodynamic profiling Journal of Drug Delivery Science and Technology 51, 152-163
Downloads
Published
How to Cite
Issue
Section
License
This work is licensed under a Creative Commons Attribution 4.0 International License.
You are free to:
- Share — copy and redistribute the material in any medium or format
- Adapt — remix, transform, and build upon the material for any purpose, even commercially.
Terms:
- Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
- No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.
