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

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.

Optimally biosynthesized, PEGylated gold nanoparticles functionalized with quercetin and camptothecin enhance potential anti-inflammatory, anti-cancer and anti-angiogenic activities.

BACKGROUND: The development of nano delivery systems is rapidly emerging area of nanotechnology applications where nanomaterials (NMs) are employed to deliver therapeutic agents to specific site in a controlled manner. To accomplish this, green synthesis of NMs is widely explored as an eco-friendly method for the development of smart drug delivery system. In the recent times, use of green synthesized NMs, especially metallic NMs have fascinated the scientific community as they are excellent carriers for drugs. This work demonstrates optimized green, biogenic synthesis of gold nanoparticles (AuNPs) for functionalization with quercetin (QT) and camptothecin (CPT) to enhance potential anti-inflammatory, anti-cancer and anti-angiogenic activities of these drugs. RESULTS: Gold nanoparticles were optimally synthesized in 8 min of reaction at 90 °C, pH 6, using 4 mM of HAuCl4 and 4:1 ratio of extract: HAuCl4. Among different capping agents tested, capping of AuNPs with polyethylene glycol 9000 (PG9) was found best suited prior to functionalization. PG9 capped AuNPs were optimally functionalized with QT in 1 h reaction at 70 °C, pH 7, using 1200 ppm of QT and 1:4 ratio of AuNPs-PG9:QT whereas, CPT was best functionalized at RT in 1 h, pH 12, AuNPs-PG9:CPT ratio of 1:1, and 0.5 mM of CPT. QT functionalized AuNPs showed good anti-cancer activity (IC50 687.44 µg/mL) against MCF-7 cell line whereas test of anti-inflammatory activity also showed excellent activity (IC50 287.177 mg/L). The CAM based assessment of anti-angiogenic activity of CPT functionalized AuNPs demonstrated the inhibition of blood vessel branching confirming the anti-angiogenic effect. CONCLUSIONS: Thus, present study demonstrates that optimally synthesized biogenic AuNPs are best suited for the functionalization with drugs such as QT and CPT. The functionalization of these drugs with biogenic AuNPs enhances the potential anti-inflammatory, anti-cancer and anti-angiogenic activities of these drugs, therefore can be used in biomedical application.