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Clofazimine (CFZ) is highly active against mycobacterium, including resistant Mycobacterium tuberculosis, but its therapeutic efficacy via the oral route is limited by severe adverse effects, poor aqueous solubility, and slow onset of action. Pulmonary delivery of CFZ is an attractive alternative to target mycobacterium-harboring alveolar macrophages. This study explores the use of air jet milling to develop a respirable, cost-effective CFZ formulation. Jet milled CFZ was readily dispersed from an off-the-shelf dry powder inhaler without the need for additional excipients or carrier particles. Additionally, milled CFZ was internalized by J774.A1 alveolar macrophages within 8 h, with evidence of intracellular biotransformation of the CFZ crystals and macrophage sequestration by 24 h. Less macrophage toxicity was noted in comparison to solubilized drug. Compared to macrophage uptake rate, dissolution of milled CFZ was limited, thereby potentially reducing systemic absorption and subsequent side effects. These results suggest that jet milling is an effective manufacturing method in the development of a CFZ formulation for pulmonary delivery and alveolar macrophage targeting.

The aim and objective of the present study was to formulate and evaluate controlled release polymeric tablets of ibuprofen with determinations of formulation factors using various grades and types of polymer ethocel i.e. ethocel standard 10P; 10FP, 100P and100FP for their release rates and release patterns in suitable media and also the mechanism involved in the release of drug from the matrices. The effect of several co-excipients was also studied on the drug release rates and patterns of Ibuprofen from the polymeric matrices. Ibuprofen-ethocel CR tablets were prepared at three different D: P ratios i.e. 10:1, 10:2 and 10:3. The effects of co-excipients were studied only in formulations having D: P ratio of 10:3. In vitro drug release studies of ibuprofen-ethocel controlled release matrix tablets were carried out in phosphate buffer pH 6.8 using pharma test dissolution apparatus adopting rotating basket method according to USP. Different kinetic models were applied to the release data of test formulations in order to investigate the release mechanism of drug from the controlled release matrix tablets. The release patterns of ibuprofen-ethocel CR matrices were compared with reference conventional ibuprofen tablets and ibuprofen SR tablets. F2 similarity factor was applied to the test formulations and reference standard to compare their similarities. The drug formulations studied exhibited satisfactory release results.

The aim of the present study was the formulation and evaluation of controlled release polymeric tablets of Diclofenac Potassium by wet granulation method for the release rate, release pattern and the mechanism involved in drug release. Formulations having three grades of polymer Ethocel (7P; 7FP, 10P, 10FP, 100P, 100FP) in several drugs to polymer ratios (10:3 and 10:1) were compressed into tablets using wet granulation method. Co-excipients were added to some selected formulations to investigate their enhancement effect on in vitro drug release patterns. In vitro drug release studies were performed using USP Method-1 (Rotating Basket method) and Phosphate buffer (pH 7.4) was used as a dissolution medium. The similarities and dissimilarities of release profiles of test formulations with reference standard were checked using f2 similarity factor and f1 dissimilarity factor. Mathematical/Kinetic models were employed to determine the release mechanism and drug release kinetics.

Being controlled release dosage forms, tablets allow an improved absorption and release profiles of Ofloxacin. The fact that drugs with fine particles size can be compressed well after wetting, so in our research studies Ofloxacin controlled release matrix tablets were prepared by wet granulation technique. In order to investigate the potential of Ethyl cellulose ether derivatives as a matrix material, Ofloxacin formulations with different types and grades of Ethocel were prepared at several drug-to-polymer ratios. The method adopted for in vitro drug release studies was USP Method-1 (rotating Basket Method) by Pharma test dissolution apparatus using phosphate buffer 7.4 pH as a dissolution medium. Various Kinetic models were employed to the formulations for the purpose of determination of release mechanism. A comparative study was performed between the tested Ofloxacin-Ethocel formulations and a standard reference obtained from the local market. F1 dissimilarity factor and f2 similarity factor were applied to the formulations for the checking of dissimilarities and similarities between the tested formulations and reference standard.