: Cancer and tumor has been major reasons for numerous deaths in this century across the world. Many strategies have been designed to treat, diagnose or prevent cancer. The success of the chemotherapy largely depends on the drug targeting. The advent of nanotechnology has vastly improved the drug delivery for targeting and diagnosis. Nevertheless, the accuracy of drug targeting with polymeric nanoparticles has always been questionable. The polymeric nanoparticles synthesised from varieties of lipid based compounds or combined with vectors such as liposomes, ethosomes, and transferosomes may allow the drug to overcome the issue of resistance to drug absorption in biological membranes. The combined effects of lipid based nanocarriers is known to improve the efficacy and accuracy of polymeric nanoparticles. The present review explores the application of lipid based nano carriers in treatment. A special focus is given to the use of lipid based nanocarriers in the treatment, diagnosis and mitigation of cancer located in blood, brain, lung and colon. The treatment of these cancers has always been questionable as the chances of relapse is very high. The review encompasses the use of lipid based nanocarriers in targeting tissue specific cancer cells.
Background: According to the global cancer report of 2019, the burden of cancer will exceed more than 18 million becoming one of the major causes of global mortality rate. There is a pressing need to establish novel drug candidates for cancer treatment, though many anticancer agents are available in the market owing to their adverse effects. In recent years, quinazoline and its derivatives have been considered as a novel class of cancer chemotherapeutic agents that show promising activity against different tumors. Objective: The objective of this study is to evaluate the anti-cancer potential of the novel class of quinazoline tethered acetamide derivatives against six different cancer cell lines. Method: A novel series of various substituted quinazolinone acetamides were synthesized through a feasible scheme. The synthetic scheme involves the conversion of benzoxazinone (from anthranilic acid and benzoyl chloride) intermediate to 3-amino quinazoline-4-one which is further converted to the final amide by tethering with the propionyl chloride employing Schotten-Baumann Reaction conditions. All the synthesized derivatives characterized by IR, 1HNMR and MASS spectral methods and anti-cancer activity evaluated by employing MTT assay for six cancer cell lines and one normal human cell line. Results: All the synthesized compounds were screened for anti-cancer activity against six cancer cell lines, including A 549 (lung), DU 145 (prostate), HT 29 (colon), MCF-7 (breast), SiHA (cervical), B16F10 (mouse skin melanoma) and one normal human fibroblast cell lines. All the compounds displayed a decent cytotoxicity profile when compared with the standard drug, doxorubicin. Among the synthesized compounds (5a to 5n) tested, two compounds, 5f and 5g have demonstrated excellent cytotoxicity against SiHA and MCF-7 cancer cell lines. Conclusion: Comparatively, most of the compounds displayed decent cytotoxicity potential relative to the standard drug, doxorubicin. Further investigations are needed to establish the detailed mechanism of action of the developed novel quinazolinone acetamides.
The current study aimed to formulate an elementary osmotic pump (EOP) and push-pull osmotic pump (PPOP) based drug delivery system for controlled release of an anti-diabetic agent, repaglinide is expected to provide sustained release. EOP and PPOP method prepared repaglinide tablets by wet granulation technique. EOP designed 15 formulations F1-F15 and 14 formulations were done by PPOP method. All the formulations were evaluated for various physicochemical parameters and in-vitro dissolution studies. The release data was fitted into mathematical kinetic modeling studies to check the release mechanism. Further, the optimized formulations from both methods were characterized by FTIR and stability studies. EOP and PPOP methods successfully prepared repaglinide osmotic tablets. All the formulations exhibitedb satisfactory results for all evaluated parameters. The highest drug release was exhibited from F15 prepared by EOP method with 99.76% and FF14 with 15% coating prepared by PPOP method with drug release of 99.73%. Based on the in vitro dissolution profile, formulation F15 and FF14 exhibited zero-order with Korsmeyer-Peppas kinetics with Fickian diffusion-controlled release mechanism with high drug release in 24 hours and hence were selected as optimized formulations. The drug-excipient compatibility study by FTIR indicated no significant interactions between drugs and excipients. The formulations were stable after 3 months of accelerated stability studies. EOP and PPOP were designed to effectively administrate repaglinide drugs for a prolonged period of time.
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