Transdermal drug delivery influence consumer acceptance and marked increase in bioavailability of some drugs which undergoes hepatic first-pass metabolism. Fabrication of transdermal patch requires lots of attention regarding the amount of components used for it. Because of varied nature of polymer and plasticizer, transdermal patches have different properties and different drug release. This study is on the basis to evaluate the amount to be needed for fabrication of diclofenac transdermal patch. Study shows that Hydroxy Propyl Methyl Cellulose has great influence on transdermal patch, if it is used alone in combination with glycerin or PEG-4000 plasticizer.
Methotrexate is the treatment of choice for rheumatoid arthritis, having significant side effects on oral administration, prompting researchers to consider transdermal administration. Transfersomes can overcome the challenges of transdermal administration of drugs because of their deformable nature, allowing for greater skin penetration than other formulations. However, due to an enormous number of product and process variables, the manufacturing of transfersomes proved a pain. The goal of the research study was to use a Plackett‐Burman design to evaluate an important product and process variables connected with the preparation of methotrexate transfersomes. The influence of six product and process variables on %entrapment efficiency and vesicle deformability was investigated and according to p‐values, and the Pareto chart, the concentration of lipid, edge activator, and methotrexate were found critical variables influencing vesicle features having positive and negative effects on variables. In the future, experimental design may be used to optimize these critical parameters for further exploration in the development of methotrexate transfersomes.
Background: Alcohol induced dose dumping is a noteworthy question in designing of modified release dosage forms and it led the marketed products withdrawal by regulatory agencies. Diltiazem HCl is a highly watersoluble drug and may undergo faster dissolution in presence of alcohol. The purpose of the present study was to develop extended-release tablets of Diltiazem HCl tablets by direct compression method having robustness in hydro-alcoholic media. Materials and Methods: Using QbD approach, lubricants and polymer as CMAs and drug release as CQAs were identified and further optimization was done by employing 3 2 factorial design. The extended-release tablets were evaluated for hardness, friability, weight variation and dissolution study was performed in 40% Alcoholic Phosphate buffer pH 5.8. Results: The scientific finding reveals that the concentration of HPMC K-100M DC (12%) and xanthan gums (12%) are capable of providing extended release of drug till the end of 12 hr in pH 5.8 phosphate buffer as well as in 40% Alcoholic Phosphate buffer pH 5.8. Conclusion: These results showed a robust in-vitro drug release profile when exposed to hydro-alcoholic media till 12 hr. Formulation was subjected to accelerated condition for stability testing and was found satisfactory.
Methotrexate on its oral and intravenous administration results in unwanted adverse effects. This drawback can be overcome by transdermal delivery because of its painless objective for systemic drug administration. Transfersomes are ultra-deformable vesicles with the flexibility to reach deeper tissues of the skin. The objective of this research work was to develop methotrexate transfersomal gel by thin film hydration technique, evaluated for entrapment efficiency, deformability, mean vesicle size, and stability, and incorporated into carbopol gel for ease of handling and skin applicability for a longer period of retention on skin. MTX-TFS gel & conventional gel were characterized for consistency, transparency, viscosity, and pH. Ex-vivo skin permeation studies were performed using abdominal goat skin and drug release kinetic parameters and transdermal flux were calculated using mathematical models. The results indicate that MTX was successfully entrapped (84.77 ± 2.35 %w/w) in transfersomes having 240±1.6 nm vesicle sizes and 27.13±0.7 deformability index. The gel was permeated through the skin at a rate of 28.12±2.58 µg/cm 2 /hr as compared to the conventional gel (10.35±2.14 µg/cm 2 / hr). From the study, it was concluded that the MTX-TFS gel can be used as a possible substitute for the conventional formulation for transdermal drug delivery due to 3 times improvement in transdermal flux.
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