Engineering the liposomal formulations from natural peanut phospholipids for pH and temperature sensitive release of folic acid, levodopa and camptothecin

Abstract

The present study demonstrates the extraction and identification of phospholipids (PLs) from peanut seed for formulation of liposomes for pH and thermo-sensitive delivery and release of folic acid (FA), levodopa (DOPA) and, camptothecin (CPT). The TLC, FTIR and GC-MS based characterization of extracted peanut PLs showed phosphatidylethanolamine, cardiolipin and phosphatidic acid as major PLs and palmitic acid and oleic acid as major fatty acids. Liposomes (LSMs) of size 1-2 μm formulated by optimized thin-film hydration method were found to entrap FA, DOPA and CPT with 58, 61.4 and 52.12% efficiency, respectively with good stability. The effect of external stimuli like pH and temperature on the release pattern of FA, DOPA and CPT indicated that FA was optimally released at pH 10 and 57 °C, DOPA at pH 2 and 37 °C, while CPT was best released at pH 6 and 47 °C. When tested for the in vitro activity, DOPA released by DOPA@LSMs showed lower toxicity to 3T3 than to SH-SY5Y cells. Similarly, CPT released by CPT@LSMs showed remarkable anticancer activity against MCF-7 cells with an IC50 value of 17.99 μg/mL. Thus peanut PLs can be efficiently used for liposomal formulations for pH and thermo-sensitive release of drugs.

Keywords: Camptothecin; In vitro drug release; Liposomes; Parkinson's disease; Phospholipids.