Faculty of Pharmacy, Damascus University, Damascus, Syria.
Sci Rep. 2021 Dec 2;11(1):23345. doi: 10.1038/s41598-021-02826-7.
The aim of the present study was to formulate clindamycin (CLN) as a microsponge based gel to release the drug in a controlled manner and reduce the side effects in the treatment of acne. Since this method requires poor water solubility of the drug to be loaded in particles, therefore, conversion of the hydrochloride salt to free base was done. By using an emulsion solvent diffusion method, we made six different formulations of microsponges containing CLN-free base by changing the proportions of polymer, emulsifier and the pH of the external phase. These formulations were studied for physical characterization and for drug- polymer interactions. The physical characterization showed that microsponge formulations coded by C5, C6 resulted in a better loading efficiency and production yield and their particle size was less than 30 µm. Scanning electron microscopy images showed the microsponges porous and spherical. C5, C6 microsponge formulation was prepared as gel in Carbopol and in vitro evaluated. The microsponge formulation gel C8 was found to be optimized. C8 released 90.38% of drug over 12 h and showed viscosity 20,157 ± 38 cp, pH of 6.3 ± 0.09 and drug content of 99.64 ± 0.04%. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed no significant interactions between excipients and drug.
本研究的目的是将克林霉素（CLN）制成微海绵凝胶，以控制药物释放并减少治疗痤疮的副作用。由于该方法需要将药物的低水溶性负载到颗粒中，因此将盐酸盐转化为游离碱。我们使用乳化溶剂扩散法，通过改变聚合物、乳化剂和外相 pH 的比例，制备了六种不同载有 CLN 游离碱的微海绵配方。这些配方进行了物理特性研究和药物-聚合物相互作用研究。物理特性研究表明，编码为 C5 和 C6 的微海绵配方具有更好的载药效率和产率，且粒径小于 30µm。扫描电子显微镜图像显示微海绵具有多孔和球形结构。C5 和 C6 微海绵配方被制备成 Carbopol 凝胶并进行了体外评估。发现微海绵配方凝胶 C8 是优化的。C8 在 12 小时内释放了 90.38%的药物，显示出粘度为 20,157±38cp、pH 值为 6.3±0.09 和药物含量为 99.64±0.04%。傅里叶变换红外光谱和差示扫描量热法证实赋形剂和药物之间没有明显的相互作用。
