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This research work aimed to target the early morning peak symptoms of chronic stable angina through formulating antianginal drug, Trimetazidine (TMZ) in a pulsatile-release tablet.
The core formulae were optimized using 22.31 factorial design to minimize disintegration time (DT) and maximize drug release after 5 minutes (Q5min). Different ratios of Eudragit S100 and Eudragit L100 were used as a coating mixture for the selected core with or without a second coating layer of hydroxypropyl methyl cellulose (HPMC E50). The different formulation variables were statistically optimized for their effect on lag time and drug release after 7 hours (Q7h) using Box-Behnken design. The optimized formula (PO) was subjected to stability study and pharmacokinetic assessment on New Zealand rabbits.
The optimal core (F8) was found to have 1.76 min disintegration time and 61.45% Q5min PO showed a lag time of 6.17 h with 94.80% Q7h and retained good stability over three months. The pharmacokinetic study confirmed the pulsatile-release pattern with Cmax of 206.19 ng/ml at 5.33 h (Tmax), as well as 95.85% relative bioavailability compared to TMZ solution.
Overall pulsatile-release tablets of TMZ succeeded in releasing the drug rapidly after a desirable lag time, providing a promising approach for early morning anginal symptoms relief.
Overall pulsatile-release tablets of TMZ succeeded in releasing the drug rapidly after a desirable lag time, providing a promising approach for early morning anginal symptoms relief.
Lipid nanocarriers have been widely tested as drug delivery systems to treat diseases due to their bioavailability, controlled release, and low toxicity. For the pulmonary route, the Food and Drug Administration favors the use of substances generally recognized as safe, as well as biodegradable and biocompatible to minimize the possibility of toxicity. Tuberculosis (TB) remains a public health threat worldwide, mainly due to the long treatment duration and adverse effects. Therefore, new drug delivery systems to treat TB are needed.
Physicochemical characterization of different lipid-based nanocarriers was used to optimize carrier properties. Optimized systems were incubated with Mycobacterium tuberculosis to assess whether lipid-based systems act as an energy source for the bacteria, which could be counterproductive to therapy.
Several excipients and surfactants were evaluated to prepare different types of nanocarriers using high-pressure homogenization.
A mixture of trimyristin with castor oil was chosen as the lipid matrix after differential scanning calorimetry analysis. A mixture of egg lecithin and PEG-660 stearate was selected as an optimal surfactant system as this mixture formed the most stable formulations. Nab-Paclitaxel in vivo Three types of lipid nanocarriers, solid lipid nanoparticles, nanostructured lipid carriers (NLC), and Nano emulsions, were prepared, with the NLC systems showing the most suitable properties for further evaluation. It may provide the advantages of increasing the entrapment efficiency, drug release, and the ability to be lyophilized, producing powder for pulmonary administration being an alternative to entrap poor water-soluble molecules.
Furthermore, the NLC system can be considered for use as a platform for the treatment of TB by the pulmonary route.
Furthermore, the NLC system can be considered for use as a platform for the treatment of TB by the pulmonary route.
This study is focused on preparing rifampicin loaded bovine serum albumin nanoparticles (RIF BSA NPs) suitable for intravenous application using systematic quality by design (QbD) approach.
Rifampicin is one of the first line drugs used for tuberculosis therapy. The therapy lasts for a long time. Thus, there is a need to develop sustained release formulation of rifampicin for intravenous application.
The main objective of this study is optimizing particle size and entrapment efficiency of rifampicin loaded bovine serum albumin nanoparticles (RIF BSA NPs) and making it suitable for intravenous application using QbD approach.
Quality target product profile was defined along with critical quality attributes (CQAs) for the formulation. 32 factorial design was used for achieving the predetermined values of CQAs, i.e., mean particle size <200 nm and percent entrapment efficiency>50%. Incubation time of drug with colloidal albumin solution and ratio of rifampicin albumin, were selected as independent variables. Check point analysis was performed to confirm the suitability of regression model for optimization.
The optimized RIF BSA NPs were characterized by FTIR, DSC, 1H NMR techniques. The NPs observed by transmission electron microscopy were spherical in shape. The rifampicin release could be sustained for 72 hours from BSA NPs matrix. RIF BSA NPs dispersion was stable at 5 ± 3°C for 72 hours. Non-toxicity of nanoparticles to RAW 264.7 cell line was proved by MTT assay.
Development of RIF BSA NPs with desired quality attributes was possible by implementing QbD approach. The optimized formulation suitable for intravenous application can potentially improve the therapeutic benefits of rifampicin.
Development of RIF BSA NPs with desired quality attributes was possible by implementing QbD approach. The optimized formulation suitable for intravenous application can potentially improve the therapeutic benefits of rifampicin.
Despite exhibiting promising anticancer potential, the clinical significance of capecitabine (a potent prodrug of 5-fluorouracil used for treatment of colorectal cancer) is limited owing to its acidic and enzymatic hydrolysis, lower absorption following the oral administration, poor bioavailability, short plasma half-life and poor patient compliance.
The present study was aimed to fabricate the capecitabine as smart pH-responsive hydrogel network to efficiently facilitate its oral delivery while shielding its stability in the gastric media.
The smart pH sensitive HP-β-CD/agarose-g-poly(MAA) hydrogel network was developed using an aqueous free radical polymerization technique. The developed hydrogels were characterized for drug-loading efficiency, structural and compositional features, thermal stability, swelling behaviour, morphology, physical form, and release kinetics. The pH-responsive behaviour of developed hydrogels was established by conducting the swelling and release behaviour at different pH values (1.