Purpose

Fat from Capra hircus (goat fat) has been widely used for drug delivery.

Methods

In this work, 1:1, 1:2, and 2:1 of goat fat and Softisan® 142 were melted together, cooled at room temperature, and the resultant matrix further modified with Phospholipon 90G (4:1) to obtain solidified reverse micellar solutions (SRMS). SRMS were used to prepare solid lipid microparticles (SLMs) loaded with or without glibenclamide, a poorly water soluble antidiabetic drug by hot melt homogenization. Particle size, morphology, thermal behavior, drug encapsulation efficiency, in vitro release study, and in vivo fate in diabetogenic rats were investigated.

Results

We report here an improved drug holding capacity (70.35%) of the lipid matrix of SRMS 2:1 due to imperfection of the lipid mixtures showing lower transition temperatures (117.0 °C) and enthalpies (−12.5 mW/mg). In vitro drug diffusion showed 66.98% drug release from SLM 2:1 exhibiting non-Fickian diffusion model (anomalous behavior) and almost zero-order kinetic. SLM 2:1 also gradually released 56.98% of glibenclamide under 16 h and maintained a steady state till 24 h; generally lowering blood glucose from 600 to 120 mg/dL unlike SLM 1:2 which showed burst glibenclamide release of 22.66% within 30 min with consequent rise in blood sugar.

Conclusion

The 2:1 micellar solution (SRMS) of homolipids could deliver glibenclamide in a sustained form better than the conventional tablet form.

中文翻译：

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均质胶束溶液中缓释释放的格列本脲负载的固体脂质微粒

目的

从脂肪山羊属（山羊脂肪）已被广泛用于药物递送。

方法

在这项工作中，将山羊脂肪与142的1：1、1：2和2：1融化在一起，在室温下冷却，然后将所得基质进一步用磷脂90G（4：1）改性以获得固化的可逆胶体。胶束溶液（SRMS）。SRMS用于通过热熔均质来制备带有或不带有格列本脲（水溶性差的抗糖尿病药物）的固体脂质微粒（SLM）。研究了糖尿病大鼠的粒径，形态，热行为，药物包封效率，体外释放研究和体内命运。

结果

我们在这里报告了SRMS 2：1脂质基质的改善的药物保持能力（70.35％），这是由于脂质混合物的缺陷所致，它们显示出较低的转变温度（117.0°C）和焓（-12.5 mW / mg）。体外药物扩散显示SLM 2：1释放66.98％的药物，表现出非菲克扩散模型（异常行为）和几乎零级动力学。SLM 2：1在16小时内也逐渐释放了56.98％的格列本脲，并一直保持稳定状态直到24小时。通常将血糖从600毫克/分升降低到120毫克/分升，这与SLM 1：2不同，后者显示30分钟内格列本脲突然释放22.66％，从而导致血糖​​升高。

结论

同源脂质的2：1胶束溶液（SRMS）可以比常规片剂形式更好地持续递送格列本脲。