Biopharmaceutics and Pharmacokinetic Division, Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Biopharmaceutics and Pharmacokinetic Division, Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Int J Pharm. 2014 Jan 1;459(1-2):30-9. doi: 10.1016/j.ijpharm.2013.11.011. Epub 2013 Nov 13.
Mixed drug delivery systems possess advantages over discrete systems, and can be used as a strategy to design more effective formulations. They are more valuable if the embedded particles perform well, rather than using drugs that have been affected by the surrounding vehicle. In order to address this concept, different liposomes have been incorporated into hydrogel to evaluate the potential effect on the controlled release of liposomes. Radiolabeled liposomes, with respect to different acyl chain lengths (DMPC, DPPC, or DSPC) and charges (neutral, negative [DSPG], or positive [DOTAP]) were integrated into chitosan-glycerophosphate. The results obtained from the biodistribution showed that the DSPC liposomes had the highest area under the curve (AUC) values, both in the blood (206.5%ID/gh(-1)) and peritoneum (622.3%ID/gh(-1)), when compared to the DPPC and DMPC formulations, whether in liposomal hydrogel or dispersion. Interesting results were observed in that the hydrogel could reverse the peritoneal retention of negatively charged liposomes, increasing to 8 times its AUC value, to attain the highest amount among all formulations. The interactions between the liposomes and chitosan-glycerophosphate, confirmed by the Fourier transform infrared (FTIR) spectra as shifted characteristic peaks, were observed in the combined systems. Overall, the hydrogel could control the release of intact liposomes, which could be manipulated by both the liposome type and interactions between the two vehicles.
混合药物传递系统具有优于离散系统的优势，可作为设计更有效配方的策略。如果嵌入的颗粒表现良好，则比使用受周围载体影响的药物更有价值。为了解决这个概念，已经将不同的脂质体纳入水凝胶中，以评估其对脂质体控制释放的潜在影响。放射性标记的脂质体，具有不同的酰基链长度（DMPC、DPPC 或 DSPC）和电荷（中性、负[DSPG]或正[DOTAP]），已整合到壳聚糖-甘油磷酸酯中。从生物分布获得的结果表明，DSPC 脂质体在血液（206.5%ID/gh(-1)）和腹膜（622.3%ID/gh(-1)）中的曲线下面积（AUC）值最高，与 DPPC 和 DMPC 制剂相比，无论是在脂质体水凝胶还是分散体中。有趣的结果是观察到水凝胶可以逆转带负电荷的脂质体在腹膜中的保留，将其 AUC 值增加到 8 倍，达到所有制剂中最高的含量。脂质体和壳聚糖-甘油磷酸酯之间的相互作用，如特征峰的位移，通过傅里叶变换红外（FTIR）光谱得到证实，在组合系统中观察到。总的来说，水凝胶可以控制完整脂质体的释放，这可以通过脂质体类型和两种载体之间的相互作用来操纵。
