International Journal of Drug Delivery

Preparation and Evaluation of 5 Fluorouracil solid dispersion formulations for therapeutic management of colorectal cancer (CRC)

2022-03-05T22:06:41+0530

Background A solid dispersion formulation (SD) involves dispersion of poor water soluble active pharmaceutical ingredients (API) in a solubility enhancing polymer with the uttermost goal of improving the oral bioavailability of the API. Objective This study is aimed at production and evaluation of 5- Fluorouracil (5- FU) SD formulations for colon delivery using the hot met technique. Method The solid dispersions of 5-FU were prepared by hot melting method; The SD formulations were characterized using a scanning electron microscopy, USP dissolution apparatus type 2, and MTT assay. Results The SEM revealed that all SD formulations particles were in amorphous state, they rod like shaped with size ranging between 98 -112µm. The FTIR spectral show no chemical interactions between the excipients and 5 FU. The yield (PY), drug entrapment efficiency (DEE) and the drug loading (DL) values were high enough to support commercial scale up of the technique. SD2 had the highest DEE, cumulative drug released and DL values. This may be responsive for its improved cytotoxicity against HT115 cells. The releases of 5 FU in all the formulations follow both Fickian´s and non-Fickian´s kinetics which are also pH responsive with no sign of dose dumping. Conclusion This study demonstrated successful production of pH responsive 5 FU solid dispersions, by hot melt technique. The release follows Korymeyer –Peppas kinetic models and selectively delivered 5 FU to the colon which improved cytotoxicity activity against CRC.

Evaluation of anti-hyperlipidemic activity in high fat diet induced hyperlipidemic rats of Carissa carandas (Auct.) leaves extract

2022-03-05T22:08:42+0530

Hyperlipidemia contributes significantly in the manifestation and development of atherosclerosis and heart disease. Although synthetic lipid‑lowering drugs are useful in treating hyperlipidemia, there are number of adverse effects. Therefore, the current interest has stimulated the search for new lipid‑lowering agents with minimal side effects from natural sources. The Purpose of this study was to examine the lipid lowering capability of aqueous: ethanol (1:1) extract of Carissa carandas in high fat diet induced hyperlipidemic rats. A highly significant increase in the weight of high cholesterol diet rats was observed when compared with control group (P<0.01). The extract caused a significant reduction in body weight, Cholesterol, Triglycerides, HDL and LDL in hyperlipidemic rats. Histopathological changes induced by high cholesterol diet were also significantly reduced by the extract. The activity of ethanol and water extract of C. carandas was comparable to that of atorvastatin.

Gastro-protective effect of some statins against induced gastric ulcer in rats

2022-03-05T22:11:06+0530

Abstract Background & Objective: The objective of the present study was to evaluate the effect of different statins (HMG-CoA reductase inhibitors) on gastric and duodenal ulcer in rats. Methods: The effect of different statins on gastric and duodenal ulcers were evaluated by using different experimental models such as acetic acid induced chronic gastric ulcer, pylorus ligation induced gastric ulcer, ethanol induced gastric ulcer, stress induced gastric ulcer and cysteamine induced duodenal ulcer. Results: The different statins tested in the present showed variable effects in different models of gastric ulcers and cysteamine induced duodenal ulcer. Atorvastain showed anti-ulcer activity in three models; pylorus ligation, ethanol induced gastric ulcer and acetic acid induced chronic gastric ulcers. Simvastatin showed a decrease in free acidity in pylorus ligated rats while lovastatin did not influence gastric and duodenal ulcer formation or healing of gastric ulcers. Interpretation & Conclusion: The atorvastatin showed significant effect on the healing and development of gastric ulcers while other statins did not influence ulcer healing or ulcer formation. It was concluded atorvastatin possess anti-ulcer effect in rats and all the tested statins may be safe for administration to patients suffering from peptic ulcer disease.