Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt; Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj, 11942, Saudi Arabia.
Colloids Surf B Biointerfaces. 2020 Sep;193:111046. doi: 10.1016/j.colsurfb.2020.111046. Epub 2020 May 1.
The purpose of this study was to develop miconazole nitrate (MN) based solid lipid nano-carrier formulae for topical delivery to enhance its antifungal effectiveness. Miconazole nitrate loaded Solid lipid nanoparticles (MN-SLNs) were formulated using a high shear homogenization technique characterized by particle size, polydispersity index (PI), trapping efficiency (EE percent), drug loading (DL percent) and zeta potential (ZP) characteristics. Furthermore, the optimized formulae were investigated for in-vitro release, ex-vivo study, skin toxicity test, and antifungal activity. With a particle size range of 244.2 ± 27.2 nm to 493.6 ± 35.3 nm, the selected MN-SLNs were spherical shaped. A high EE product percentage ranging from 79.38 ± 2.35 percent to 95.92 ± 6.12 percent and Zeta potential ZP values ranging from-21.6 ± 7.05 mV to-31.4 ± 6.84 mV suggesting strong stability was achieved. A controlled release of MN from the SLNs up to 48 h was shown in-vitro release study. The ex-vivo study showed that the selected MN-SLN (F4) mixture exhibited higher MN flux in the skin than a 1% MN solution. Moreover, selected MN-SLN (F4) has demonstrated a higher zone of inhibition against Candida albicans than a simple drug solution. MN-SLN (F4) had the lowest toxicity value for the skin. Besides, the MN-SLNs (F4) substantially reported antifungal activity with the least histopathological improvements compared to MN-solution utilizing immune-suppressing albino rats with induced candidiasis fungal infection. It can be fulfilled that SLNs can be acquired as a promising carrier for topical delivery of poorly soluble MN.
本研究旨在开发硝酸咪康唑（MN）的固体脂质纳米载体配方，用于局部递药以提高其抗真菌效果。采用高剪切匀化技术制备载硝酸咪康唑的固体脂质纳米粒（MN-SLNs），并对其粒径、多分散指数（PI）、包封率（EE%）、载药量（DL%）和 Zeta 电位（ZP）等特性进行了表征。此外，还对优化后的配方进行了体外释放、离体研究、皮肤毒性试验和抗真菌活性研究。所选 MN-SLNs 的粒径范围为 244.2±27.2nm 至 493.6±35.3nm，呈球形。EE%在 79.38±2.35%至 95.92±6.12%之间，ZP 值在-21.6±7.05mV 至-31.4±6.84mV 之间，表明稳定性较强。体外释放研究表明 MN 从 SLNs 中呈控制释放，可持续 48h。离体研究表明，所选 MN-SLN（F4）混合物在皮肤中的 MN 通量高于 1%MN 溶液。此外，与简单药物溶液相比，所选 MN-SLN（F4）对白色念珠菌的抑制区更大。MN-SLN（F4）对皮肤的毒性值最低。此外，MN-SLNs（F4）在免疫抑制白化大鼠诱导的念珠菌真菌感染模型中，与 MN 溶液相比，显示出更好的抗真菌活性，组织病理学改善最小。结果表明，SLNs 可作为一种有前途的载体，用于局部递药，以提高难溶性 MN 的溶解度。
