Purpose

The objective of the present study was to screen oils and suspending agents for the formulation of novel progesterone (PGT) suspension, demonstrating improved solubility, drug release, stability, and non-allergenicity. Presumably, formulated novel PGT suspensions could supersede clinically available peanut oil and lecithin based formulations (PL).

Method

The PGT suspensions were formulated by the trituration method using a vehicle (Moringa oil/peanut oil/sesame oil/sunflower oil) and a suspending agent (Neusilin US2/Fujicalin/Lecithin/Syloid 244) separately. A total of 16 PGT suspensions were evaluated for particle size, zeta potential, sedimentation, thixotropy, stability, in vitro dissolution, and allergenicity. Indeed, in silico studies were performed to elucidate interactions between principal components of the suspension, using software V. life MDS 4. 6.

Results

Findings revealed the highest PGT solubility and high viscosity in Moringa oil-based formulations. Suspensions comprising Moringa oil and Neusilin US2 (MN) exhibited the lowest suspensiod size (48.7 nm), least sedimentation rate, highest zeta potential (− 39.8), and dilatent flow behavior. The in vitro percent cumulative PGT dissolved was significantly high (94.82 ± 2.56%) from MN vis PL (52.68 ± 2.62%), at p < 0.05. In silico studies revealed strong hydrophobic and Van der Waals interactions between PGT, Moringa oil, and Neusilin US2, compared with others. Allergenicity study confirmed the superiority of Moringa oil over peanut oil (p < 0.01).

Conclusion

Moringa oil-based PGT formulations containing Neusilin US2 could be a better alternative to clinically available peanut oil and lecithin-based suspensions. Additionally, in silico interaction tools can be effectively employed for the prediction of stability and performance of suspensions.

中文翻译：

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利用辣木油和新硅素US2开发孕酮油性悬浮液

目的

本研究的目的是筛选用于配制新型孕酮（PGT）悬浮液的油和悬浮剂，证明其溶解性，药物释放，稳定性和非过敏性得到改善。据推测，配制的新型PGT悬浮液可以取代临床上可获得的花生油和卵磷脂基制剂（PL）。

方法

通过使用载体（辣木油/花生油/芝麻油/向日葵油）和悬浮剂（Neusilin US2 / Fujicalin /卵磷脂/ Syloid 244）的磨碎方法分别配制PGT悬浮液。总共评估了16种PGT悬浮液的粒径，ζ电势，沉降，触变性，稳定性，体外溶出度和致敏性。实际上，已使用软件V.life MDS 4.进行了计算机模拟研究，以阐明悬浮液主要成分之间的相互作用。

结果

研究结果表明，辣木油基配方中PGT的溶解度最高，粘度较高。包含辣木油和Neusilin US2（MN）的悬浮液表现出最低的悬浮液大小（48.7 nm），最小的沉淀速率，最高的Zeta电位（− 39.8）和流动性差。相对于MN与PL（52.68±2.62％），体外溶解的PGT累积溶解百分数显着较高（94.82±2.56％），p  <0.05。在计算机研究中，与其他相比，PGT，辣木油和Neusilin US2之间具有很强的疏水和范德华相互作用。致敏性研究证实了辣木油优于花生油（p  <0.01）。

结论

含有Neusilin US2的辣木油基PGT制剂可能是临床上可利用的花生油和卵磷脂悬浮液的更好替代品。此外，计算机交互工具可以有效地用于预测悬浮液的稳定性和性能。