Formulation and In Vitro Evaluation of a Ramipril Entrapped in a Microsponge-based Drug-delivery System.

Microsponges are porous cross-linked polymers, which have the ability to load a wide range of pharmaceutical active ingredients. They are used topically for long-term treatment applications in addition to the oral route of administration. They are characterized by the efficient distribution of active ingredients, which are loaded at a low quantity to release the drug over longer periods of time by altering the release characteristics. The objective of this study was to develop a novel drug-delivery system that included ramipril microsponges. Ramipril is an antihypertensive drug used in the treatment of elevated blood pressure. It has about 28% oral bioavailability and is eliminated through the kidneys. When administered in an instant dosage form, this medicine produces several side effects, including postural hypotension, hyperkalemia, and angioedema. Included in this study were six distinct formulas of microsponges containing ramipril and Eudragit L 100 at varied ratios that were prepared by using the Quasi-emulsion solvent diffusion technique to avoid side effects. The particle size and physical characteristics of these formulations were investigated. The effects of the polymer/drug ratio on the physical features of a microsponge's physical and compatibility study was performed by using the Fourier transform infrared spectroscopy, differential scanning calorimetry, loading efficiency, surface morphology, and particle sizes. In addition, an in vitro drug-release profile was conducted. The physical characterization showed that the loading efficiency and production yield were both improved for microsponge formulation F1. In vitro dissolution studies were performed on all formulations, and the findings were analyzed kinetically, revealing that the ramipril release rate was altered in all formulations. This study offers a new medication delivery method based on microsponge technology.

Formulation and characterization of orodispersible tablet of glimepiride.

The present study is regarding, Glimepiride is one derivatives of sulfonyl urea used in the treatment of Type II DM which classified as class-II (BCS) of high permeability and low degree of solubility. The endeavor is to improve its solubility by solvent vaporization method to enhance the rate of dissolution of glimepiride. Soluplus (Polyvinyl caprolactampolyvinyl acetate-polyethylene glycol graft co-polymer), PVP k40 (Polyvinylpyrrolidone) and PEG k5 are blended with the drug in various proportions (1:1,1:3) and prepared Soluplus1, Soluplus2, PEG1, PEG2, PVP1 and PVP2 as solid dispersion. The optimized formula of solid dispersion PVP1 is added to sodium starch glycolate and cross-carmellose. The disintegration profile will appear diminished in the drug release from the dosage form at a determined period of time. Differential scanning calorimetry appeared to a reduction in its crystallinity in solid dispersions. Scanning electron microscope and particle size analysis show a reduction in the drug particle size as solid dispersions. Fourier transform infrared spectroscopy does not show an interaction between them. Hence, that PVP1 batch will be considered from nine oral dissolving tablets dosage form. Finally, orally disintegrating tablets are estimated for various parameters; for instance, disintegration time, the content of the drug, wetting time, and in vitro release profile show a conventional result. The selected formula F6 shows a good result in disintegration time during 13-second and in-vitro drug release profile achieves 96% at the end of 40 minutes.

The Autophagy-Inducing Mechanisms of Vitexin, Cinobufacini, and Physalis alkekengi Hydroalcoholic Extract against Breast Cancer in vitro and in vivo.

OBJECTIVES: Owing to inefficiency of chemotherapy towards cancer treatment, formulation and application of herbal drug compounds will open new avenues with this regard. In this study, the anticancer effects of itexin, cinobufacini, and Physalis alkekengi (P. alkekengi) were assessed. METHODS: Herein, synergistic effects of vitexin, cinobufacini, and P. alkekengi hydroalcoholic extract were assessed against estrogen-receptor (EGFR2)-positive breast cancer mouse model. Sixty ER + breast cancer BALB/c mice (six groups each including ten members) were included. The anticancer effects of P. alkekengi hydroalcoholic extract, vitexin, and cinobufacini were administered against EGFR2 cancerous cells for 14 days. The tumor size, cytotoxic effects, and expression of Beclin-1, LC3-II, and ATG5 autophagy-related genes were investigated using RT-qPCR technique. The data was analyzed using chi-square, ANOVA, and multinomial logistic regression tests. KEY FINDINGS: The 50% lethal dose (LD50) of P. alkekengi and vitexin against the breast cancer cells included 12 mg/kg, respectively, while cinobufacini LD50 was 24 mg/kg but had no toxicity against CRL7242 breast normal cells. Furthermore, 24 mg/kg of the P. alkekengi, vitexin, and cinobufacini significantly increased the ATG5, Beclin-1, and LC3-II gene expression. CONCLUSION: Considering anticancer effects of P. alkekengi, vitexin, and cinobufacini against breast cancer through induction of the autophagy pathway, the compound formulations can be applied as anticancer therapies.