Liposomal, Ring-Opened Camptothecins with Prolonged, Site-Specific Delivery of Active Drug to Solid Tumors

A method for preparing a stable dispersion of a camptothecin, camptothecin prodrug, or analog thereof for administration to a patient in need thereof includes preparing a solution of the camptothecin, wherein the solution has a pH which places substantially an entirety of that camptothecin in a carboxylate form. The camptothecin may be a neutral camptothecin. The solution is next loaded into a liposome including at least one lipid, which may be a phospholipid. An intraliposomal pH is maintained which preserves substantially an entirety of the camptothecin in the carboxylate form. The liposomal dispersion is administered to an individual in need thereof, whereby the liposomes accumulate at and permeate into tumor tissue and an active, lactone form camptothecin is released in situ at the tumor site. Compositions formulated in accordance with the described method for treatment of a cancer in an animal in need thereof are provided also

Microfluidic manufacturing of phospholipid nanoparticles: Stability, encapsulation efficacy, and drug release

Liposomes have been the centre of attention in research due to their potential to act as drug delivery systems. Although its versatility and manufacturing processes are still not scalable and reproducible. In this study, the microfluidic method for liposomes preparation is presented. DMPC and DSPC liposomes containing two different lipid/cholesterol ratios (1:1 and 2:1) are prepared. Results from this preparation process were compared with the film hydration method in order to understand benefits and drawbacks of microfluidics. Liposomes characterisation was evaluated through stability studies, encapsulation efficacy and drug release profiles of hydrophilic and lipophilic compounds. Stability tests were performed during 3 weeks and the liposomes properties of the most stable formulations were determined using Infrared Microscopy and Atomic Force Microscopy. Microfluidic allows loading of drugs and assembly in a quick single step and the chosen flow ratio for liposomes formulation plays a fundamental role for particle sizes. One hydrophilic and one lipophilic compounds were incorporated showing how formulation and physic-chemical characteristics can influence the drug release profile