pectins and piperine

Use of natural polymer in the development of Drug Delivery Systems (DDS) has greatly increased in recent past because of their biocompatible, non-allergic and biodegradable nature. Natural polymers are usually hydrophilic supports, so in order to be a carrier of a hydrophobic drug their nature needs to be changed. Each developed system behaves differently towards different drugs in terms of loading and sustained release of the drug as well. In the present work we report differential binding of piperine & curcumin with cetyltrimethylammonium bromide (CTAB) modified cellulose, alginate and pectin. Difference in interaction between the piperine and curcumin with supports has been visualized using in-vitro as well as in-silico studies. Initial results obtained after in-silico studies have been validated via time dependent anti-trypsin, serum protein binding, anti-cathepsin, anti-oxidant, and anti-α-amylase activities. FT-IR, SEM, fluorescence and Particle size have been used to characterize the piperine loaded on CTAB-modified polymeric supports.

Topics: Alginates; Cellulose; Cetrimonium; Curcumin; Drug Carriers; Pectins; Polymers; Spectroscopy, Fourier Transform Infrared

Piperine (PIP) is a herbal drug with well-known anticancer activity against different types of cancer including hepatocellular carcinoma. However, low aqueous solubility and extensive first-pass metabolism limit its clinical use. In this study, positively charged PIP-loaded nanostructured lipid carriers (PIP-NLCs) were prepared via melt-emulsification and ultra-sonication method followed by pectin coating to get novel pectin-coated NLCs (PIP-P-NLCs) targeting hepatocellular carcinoma. Complete in vitro characterization was performed. In addition, cytotoxicity and cellular uptake of nanosystems in HepG2 cells were evaluated. Finally, in vivo anticancer activity was tested in the diethylnitrosamine-induced hepatocellular carcinoma mice model. Successful pectin coating was confirmed by an increased particle size of PIP-NLCs from 150.28 ± 2.51 nm to 205.24 ± 5.13 nm and revered Zeta potential from 33.34 ± 3.52 mV to -27.63 ± 2.05 mV. Nanosystems had high entrapment efficiency, good stability, spherical shape, and sustained drug release over 24 h. Targeted P-NLCs enhanced the cytotoxicity and cellular uptake compared to untargeted NLCs. Furthermore, PIP-P-NLCs improved in vivo anticancer effect of PIP as proved by histological examination of liver tissues, suppression of liver enzymes and oxidative stress environment in the liver, and alteration of cell cycle regulators. To conclude, PIP-P-NLCs can act as a promising approach for targeted delivery of PIP to hepatocellular carcinoma.

Topics: Alkaloids; Animals; Benzodioxoles; Carcinoma, Hepatocellular; Drug Carriers; Lipids; Liver Neoplasms; Mice; Nanostructures; Particle Size; Pectins; Piperidines; Polyunsaturated Alkamides