Objective: The aim of this study was to formulate a new developed solid dispersion (SD) containing fixed dose combination of nalidixic acid and cefdinir (500:300 mg) to improve dissolution rate of poorly soluble drugs via a new mechanism as well as the conventional mechanism of SD represented by the presence of hydrophilic carrier.Methods: Through this objective eight newly developed SD formulas of fixed dose combination of nalidixic acid and cefdinir (500:300 mg) and (polyethylene glycol 6000 and poloxamer 188) in different ratio were prepared, in addition to SD of each drug alone and simple mixture of individual SD (SMSD) prepared by means of fusion technique. Moreover, SDs beside pure drugs, simple mixture, and physical mixture (PM) were characterized by dissolution tests, solubility studies, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC), Fourier transform-infrared (FT-IR) spectroscopy and scanning electron microscopy (SEM). Results:From in vitro dissolution tests, PXRD, DSC, FT-IR, and SEM; it is indicated the presence of a physical complex between cefdinir and nalidixic acid in their SD containing combination of fixed dose of both drugs. This will affect the crystallinity of the second drug and their dissolution behavior in addition to the conventional mechanism owing to the presence of hydrophilic carrier (poloxamer 188). Conclusion:It was concluded that the newly prepared formula of SD containing fixed dose combination of nalidixic acid and cefdinir will be promising for higher dissolution profile than that from SD of each drug alone or SMSD of each drug.
Objective: The objective of the present study was to formulate niosomal formulations of benazepril hydrochloride in an attempt to overcome the hurdles associated with itʼs poor oral absorption.Methods: Nine formulations were prepared with various ratios of sorbitan monostearate (span 60), sorbitan monopalmitate (span 40) and polyoxyethylene 2 stearyl ether (brij 72) as non-ionic surfactants, cholesterol as a stabilizing agent and soya lecithin as a charge imparting agent. Then, they were characterized for vesicle size, polydispersity (PDI), entrapment efficiency (EE %), release profile, zeta (ζ) potential and transmission electron microscopy (TEM).Results: Niosomal formulations exhibited an efficient entrapment range between (80.4-97.8) percent, vesicles size analyses revealed the formation of homogenously dispersed vesicles having a size range of (3.9±1.7-8.72±4.4) micrometers. The in vitro release studies revealed that all formulations displayed sustained release in comparison with the pure drug. Formulations prepared with span 60 and span 40 possessed adequate stability according to zeta potential analysis, whereas brij 72 failed the test and possessed inadequate zeta potential range. TEM images of the optimized formulations (F7 and F8) have confirmed the formation of vesicles with spherical shapes.Conclusion: Based on the study results, niosomal formulations seem to be attractive alternatives to conventional delivery for benazepril hydrochloride.
Tamoxifen Citrate (TC) is the standard endocrine therapy for estrogen receptor (ER) positive breast cancer. TC is a selective estrogen receptor modulator (SERM) whose estrogenic properties in uterus have been linked to increased side effects like blood clots, endometrial polyps and cancer. Therefore, significant amount of research has been carried out to develop tamoxifen loaded nano-formulations with a preferential accumulation in tumor tissue rather than healthy tissues. Synthetic high-density lipoproteins (sHDL) are novel nanocarriers with inherent active-targeting ability towards tumor cells through the ligand–receptor interaction between apolipoprotein A-I (Apo A-I) and scavenger receptor class B type I (SR-BI) overexpressed in various malignant cells. The current study was carried out to investigate whether encapsulation of TC in sHDL could improve the cytotoxic effect of TC against malignant cells. For this purpose, the cytotoxicity of TC-sHDL was evaluated in MCF-7 cell line in vitro. MTT assay demonstrated the increased cytotoxicity of TC-sHDL against cancer cells as compared with the cytotoxic effect of the free drug.
Cocrystallization is an emerging approach for improving physico-chemical characteristics of an active pharmaceutical ingredient (API) for instance dissolution rate, solubility, stability in addition to mechanical properties without affecting their therapeutic activity. It is of great importance when other approaches like salt or polymorph formation do not encounter the estimated targets. In this review article, an outline of pharmaceutical cocrystals will be presented, with highlighting on factors affecting cocrystallization which include ∆pKa, donors and acceptors hydrogen bonds, molecular recognition point, synthon forming functional groups flexibility, dicarboxylic acid coformers carbon chain length and solvent effect, as well as and the methods for cocrystal preparation. Additionally, cocrystal characterization, dissolution pattern as well as the commercially available products were discussed.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.