Data for : "Scalable solvent-free production of liposomes"

This data supports work looking at scalable manufacturing of liposomes without using any solvents. This dataset contains data of particle size, PDI, zeta potential, drug release and drug loading of several formulations investigated in this paper. Abstract: Objectives. A major challenge faced with the manufacture of liposomes is the high volumes of solvents used and disposed of during manufacturing. Therefore, we have developed a solvent-free production of drug-loaded liposomes and demonstrated it applicability with both aqueous core loaded and bilayer loaded drugs. Methods. Liposomes were produced by high-shear mixing lipids in a dried powder state, followed by down-sizing of the liposomes using a Microfluidizer® processor. Liposomes were purified via tangential flow filtration and characterised in terms of size, polydispersity and drug loading. Key findings. Doxorubicin-loaded PEGylated liposomes can be manufactured using this solvent-free method with particle sizes of 100-110 nm, low PDI (<0.2) and high drug loading (97-98 %). If required, the liposomes can be further down-sized via further microfluidic processing without impacting on drug loading. Similar results were achieved with non-pegylated liposomes. With bilayer loaded amphotericin B liposomes, again liposomes could be prepared in a clinically appropriate size range (100 – 110 nm in size, low PDI) with high drug loading (98 - 100 %). Conclusions. We have demonstrated a simple and scalable solvent-free method for the production of liposomes that can be employed for both aqueous core loaded and bilayer loaded liposomes.

本数据集支撑一项关于无溶剂规模化制备脂质体（liposomes）的研究工作。本数据集包含本文所研究的多种制剂的粒径、多分散性指数（Polydispersity Index, PDI）、zeta电位（Zeta Potential）、药物释放与载药量数据。

摘要：
研究目标：脂质体制备过程中面临的核心挑战之一，是制备阶段需使用并处置大量有机溶剂。为此，我们开发了一种载药脂质体的无溶剂制备工艺，并证实该工艺可适用于水相内核载药与双层膜载药两类药物。
研究方法：将脂质以干粉状态进行高剪切混合以制备脂质体，随后借助Microfluidizer®处理器对脂质体进行粒径细化处理。通过切向流过滤对脂质体进行纯化，并对其粒径、多分散性指数与载药量进行表征。
核心研究结果：采用该无溶剂工艺可制备得到阿霉素载药聚乙二醇化脂质体（PEGylated liposomes），其粒径为100~110 nm，多分散性指数低于0.2，且载药量高达97%~98%。若有需求，可通过进一步的微流处理对脂质体进行粒径细化，且不会影响其载药量。非聚乙二醇化脂质体也可获得相近的实验结果。对于双层膜载药的两性霉素B（amphotericin B）脂质体，同样可制备得到符合临床要求的脂质体，其粒径处于100~110 nm区间，多分散性指数较低，且载药量可达98%~100%。
研究结论：本研究证实了一种简单且可规模化的脂质体无溶剂制备工艺，该工艺可同时适用于水相内核载药与双层膜载药的脂质体制备。