Intricate formulation methods and/or use of sophisticated equipment limit the prevalence of liposomal dosage-forms. Simple techniques are developed to assemble amphiphiles into globular lamellae while transiting from immiscible organic to the aqueous phase. Various parameters are optimized by injecting chloroform solution of amphiphiles into the aqueous phase and subsequent removal of the organic phase. Further simplification is achieved by reorienting amphiphiles through a spontaneous phase transition in a swirling biphasic system during evaporation of the organic phase under vacuum. Although the chloroform injection yields smaller size and PDI yet spontaneous phase transition method overrides simplicity and productivity. The size distribution of liposomes and solid/solvent ratio in both or any phases of formulation show direct relation. Surface charge dependant large unilamellar vesicles with a narrow distribution have PDI <0.4 in 10 µM saline. As small and monodisperse liposomes are prerequisites in targeted drug delivery strategies. Hence the desired size distribution <200 d.nm and PDI <0.15 is obtained through serial membrane-filtration method. Phosphatidylcholine/water 4 µmol/ml is achieved at a temperature of 10°C below the phase-transition temperature of phospholipids ensuing suitability for thermolabile entities and high entrapment efficiency. Both methods furnish the de-novo rearrangement of amphophiles into globular lamellae aiding in the larger entrapped volume. The immiscible organic phase facilitates faster and complete removable of the organic phase. High cholesterol content (55.6 mol%) imparts stability in primary hydration medium at 5+3°C for 6 months in light-protected type-1 glass vial. Collectively the reported methods are novel, scalable, time-efficient yielding high productivity in simple equipment.

中文翻译：

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氯仿注射（CI）和自发相变（SPT）是新颖的方法，简化了脂质体的制备。

复杂的配制方法和/或复杂设备的使用限制了脂质体剂型的流行。已开发出简单的技术将两亲物组装成球状薄片，同时从不混溶的有机物过渡到水相。通过将两亲物的氯仿溶液注入水相并随后除去有机相来优化各种参数。通过在真空蒸发有机相的过程中，通过旋转双相系统中的自发相变使两亲物重新定向来实现进一步的简化。尽管氯仿注射液的体积和PDI较小，但自发相变方法却超越了简单性和生产率。在制剂的两个阶段或任何阶段，脂质体的大小分布和固/溶剂比都显示出直接的关系。依赖于表面电荷的大单层囊泡，分布狭窄，在10 µM盐水中的PDI <0.4。由于小而单分散的脂质体是靶向药物递送策略的先决条件。因此，通过连续膜过滤方法获得了<200 d.nm和PDI <0.15的所需尺寸分布。在比磷脂的相变温度低10°C的温度下可实现4 mol / ml的磷脂酰胆碱/水，从而确保了对热不稳定实体的适应性和高的包封效率。两种方法都可以使两亲物从头开始重新排列成球形薄片，从而有助于更大的截留体积。不混溶的有机相有助于更快，完全除去有机相。高胆固醇含量（55。6摩尔％）可在光防护的1型玻璃小瓶中在5 + 3°C的初级水合介质中保持6个月的稳定性。集体报告的方法是新颖，可扩展，省时的方法，可在简单的设备中实现高生产率。