Lower doses of capsaicin (8-methyl-N-vanillyl-6-nonenamide) have the potential to serve as an anticancer drug, however, due to its pungency, irritant effect, poor water solubility and high distribution volume often linked to various off-target effects, its therapeutic use is limited. This study aimed to determine the biodistribution and anticancer efficacy of capsaicin loaded solid lipid nanoparticles (SLNs) in human hepatocellular carcinoma in vitro. In this study, SLNs of stearic acid loaded with capsaicin was formulated by the solvent evaporation-emulsification technique and were instantly characterized for their encapsulation efficiency, morphology, loading capacity, stability, particle size, charge and in vitro drug release profile. Synthesized SLNs were predominantly spherical, 80 nm diameter particles that proved to be biocompatible with good stability in aqueous conditions. In vivo biodistribution studies of the formulated SLNs showed that 48 h after injection in the lateral tail vein, up to 15% of the cells in the liver, 1.04% of the cells in the spleen, 3.05% of the cells in the kidneys, 3.76% of the cells in the heart, 1.31% of the cells in the lungs and 0% of the cells in the brain of rats were determined. Molecular docking studies against the identified targets in HepG2 cells showed that the capsaicin is able to bind Abelson tyrosine-protein kinase, c-Src kinase, p38 MAP kinase and VEGF-receptor. Molecular dynamic simulation showed that capsaicin-VEGF receptor complex is highly stable at 50 nano seconds. The IC50 of capsaicin loaded SLNs in HepG2 cells in vitro was 21.36 μg × ml−1. These findings suggest that capsaicin loaded SLNs are stable in circulation for a period up to 3 d, providing a controlled release of loaded capsaicin and enhanced anticancer activity.

Enhanced cancer treatment remains as one of the focused areas for researchers around the world. Hence, the progress in this direction will be a challenge and an opportunity in, inter‐disciplinary field to mitigate the suffering of millions in the upcoming decades. As we see, cancer death rate has also progressively increased despite the current impressive treatment regimens but also due to the non‐availability of vaccines and the re‐occurring of cancer in substantially recovered patients. Currently, numerous treatment strategies like surgical removal of solid tumors followed by radiation with a combination of immunotherapy/chemotherapy by the researchers and clinicians are routinely being followed. However, recurrence and distant metastasis often occur following radiation therapy, commonly due to the generation of radio‐resistance through deregulation of the cell cycle, cell death, and inhibition of DNA damage repair mechanisms. Thus, chemotherapeutic/immunotherapeutic treatment systems have progressed remarkably in the latest years owing to destroying tumors, noninvasive, and affordable charge of therapy. But, traditional chemotherapeutic approaches target the DNA of mutated and normal healthy cells, resulting in a significantly increased risk of toxicity and drug resistance. Thus, many receptors targeted therapies are in the developmental phase of discovery. Cancer cells have a specialized set of surface receptors that provide potential targets for cancer therapeutics. Cell surface receptor‐dependent endocytosis is well a known major mechanism for the internalization of macromolecular drugs. This review emphasizes the recent development of several surface receptors mediated cancer‐targeting approaches for the effective delivery of various therapeutic formulations.

Wound healing activity of the leaf extracts of Ammannia baccifera L., Lythraceae, and Blepharis maderaspatensis (L.) B.Heyne ex Roth., Acanthaceae, was investigated by excision and incision wound healing models in rats. A phytochemical screening was done to determine the major constituents of the chloroform, ethyl acetate and ethanolic fractions of ethanolic leaf extracts. The excision and incision models were used to assess the effect of the plant extracts on wound healing in rats. Phytochemical screening reveals the presence of tannins, saponins, steroids, terpenoids, and flavonoids in the extract. The wound healing effect was comparatively evaluated with a standard drug Framycetin cream. Significant wound healing activity was observed for the creams prepared with 5% ethanol fraction of B. maderaspatensis and 5% chloroform fraction of A. baccifera ethanolic leaf extracts. The results of histopathological evaluation supported the outcome of both incision and excision wound models. Ethanolic fraction of B. maderaspatensis and chloroform fraction of A. baccifera exhibited marked wound healing activity. B. maderaspatensis extract displayed a remarkable wound healing activity compared to A. baccifera.

Phytoconstituent's has significant antioxidant and anticancer activity against various types of cancer cells. But these water soluble phytoconstituent's has poor absorption due to their huge molecular size as well as it cannot be reach at the targeted disease site, thus targeted drug delivery system is one of the effective approaches to enhancing the bioavailability and decreasing drug toxicity. To achieve this target, the Proanthocyanidins (Pro) and ethyl cellulose (EC) was used to formulate nanoparticles (NPs) for effective drug delivery system. The Pro encapsulated ECNPs were formulated by simple anti-solvent particle induction method and its physico-chemical characteristics were examined by FTIR, XRD, Zeta size analyzer, SEM, and TEM. The graph theoretical network analysis was implemented to identify the drug target and subsequently molecular docking studies were screened. The identified target using graph theoretical analysis and molecular docking study reported strong interaction of Pro encapsulated ECNPs in binding pockets of MAPK. The formulated ECNPs has been very effective in arresting the proliferation of colon cancer (HT-29) cells with an IC 50 value of 33.4 μg ml −1 after 24 h treatment. Further, HT-29 cells exposure with Pro encapsulated ECNPs resulted in typical apoptotic through necrotic cellular morphology, loss of mitochondrial transmembrane potential, and high ROS generation were also observed. The observed results highlight that EC as a potential carrier material for enhancing the bioavailability of anti-cancer drugs.

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The present study evaluates anti-hyperlipidaemic and anti-atherogenic activities in Triton WR-1339 and high cholesterol diet induced hyperlipidemia in rat models. Chloroform, ethyl acetate and ethanol extracts of whole plant of Blepharis maderaspatensis were evaluated for their anti-hyperlipidaemic and anti-atherogenic activities using Triton WR-1339 induced hyperlipidaemic rats (acute study) and high cholesterol diet induced (chronic study) experimental models. Hyperlipideamia was developed by intraperitonial injection of Triton WR-1339 (200 mg/kg body weight) in acute study and feeding with cholesterol rich diet in chronic study. The animals were divided into various groups and intragastric administration of various extracts of B. maderaspatensis (100 mg/kg) body weight was given in both models. After the completion of the treatment, they were evaluated for serum total cholesterol, triglycerides, high density lipoprotein (HDL), low density lipoprotein (LDL), very low density lipoprotein (VLDL), atherogenic index (AI), coronary risk index (CRI) and were compared with the rats treated with simvastatin (20 mg/kg) of the body weight. Pre-treatment of ethanol extracts of B. maderaspatensis significantly reduced the serum total cholesterol, triglycerides, LDL, VLDL, AI and CRI as comparable with simvastatin.

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