Solidified Reverse Micellar Solution-Based Lipid Microparticles of Miconazole Nitrate: Formulation Design, Biopharmaceut
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ORIGINAL ARTICLE
Solidified Reverse Micellar Solution-Based Lipid Microparticles of Miconazole Nitrate: Formulation Design, Biopharmaceutical Characterization, and Dissolution Studies Emmanuel Uronnachi 1 & Anthony Attama 2 & Chukwuebuka Umeyor 1 & Calistus Nwakile 1 & Franklin Kenechukwu 2 & Joy Reginald-Opara 2 Accepted: 28 October 2020 # Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract Purpose The present work was aimed at formulating solidified reverse micellar microparticles (SRMMs) using templated lipids (Softisan 154, stearic acid, and Phospholipon ®90H) for improved biopharmaceutical performance, dissolution of miconazole nitrate. Methods SRMMs containing miconazole nitrate (MN) (1, 2, and 3% w/w) were formulated using Softisan® 154 (SOFT) and stearic acid (ST) and their combinations, containing Phospholipon® 90H (P90H) by melt homogenization employing Polysorbate 80 as the surfactant. The microparticles were freeze-dried, characterized, and optimized batches evaluated for in vitro dissolution in methanolic HCl and antifungal activity. Results The average SRMM yield was 70%. Entrapment efficiency and loading capacity determination showed that the lipid matrix composed of Softisan® 154 and Phospholipon® 90H (7:3) possessed greater entrapment than the other matrices with the 5% SOFT + P90H matrix containing 3% MN entrapping 98.48% of the drug. Preliminary anticandidal evaluation of the formulations showed significant activity of all the formulations containing drug. DSC analysis of the lipid excipients and matrices showed slight modifications in the physical nature of the excipients. Further analysis using X-ray diffraction showed retention of drug form in the formulations though with slight alterations in d-spacings of the X-ray diffractograms. In vitro dissolution studies of the optimized batches revealed a significant (p < 0.05) increase in dissolution rates of optimized SLM batches compared with pure MN. Kinetic modelling of the in vitro dissolution data revealed that most of the matrix systems evaluated best fitted the Korsenmeyer-Peppas model. Conclusion SRMMs improved the in vitro dissolution and antifungal activity of MN. Keywords Solid lipid microparticles . Antifungal activity . Solidified reverse micellar solution . Miconazole nitrate . Stearic acid . In vitro drug dissolution
Introduction Despite the discovery and utilization of other routes of administration, the oral route still offers the most convenient mode * Emmanuel Uronnachi [email protected] * Anthony Attama [email protected] 1
Nanomedicines and Drug Delivery Research Group, Department of Pharmaceutics and Pharmaceutical Technology, Nnamdi Azikiwe University, Awka, Anambra State 422001, Nigeria
2
Drug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State 410001, Nigeria
of drug delivery to patients due to its simplicity and ease of administration, thus enhancing patient compliance. In order to successfully and effectively delive
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