Harshitha Kumari B A

Transdermal drug delivery systems (TDDS) is a promising method of non-invasive delivery of drug molecules, and it has the following benefits: it avoids first-pass metabolism, minimizes intestinal breakdown and increases patient compliance. The stratum corneum however presents a great obstacle to drug permeation and more so on hydrophilic and high-molecular-weight drugs. More recent developments have then been directed at the inclusion of chemical permeation enhancers (CPEs) which comprise alcohols, fatty acids, terpenes and surfactants that disturb the structure of the lipids, and increases the solubility of the drug in order to enhance permeation. Simultaneously, the so-called microneedle (MN) technologies, which could be solid, coated, hollow, or dissolving, have been developed to generate the temporary microchannels in the skin and allow deep and efficient drug delivery with low discomfort and minimal damage. Effectiveness, safety, and mechanism of both CPEs and MNs were proven in preclinical trials based on rodent and porcine models, where porcine skin was also compared as a translational-friendly model known to mimic the human one. Noteworthy, the formulation of CPEs with microneedles has demonstrated the synergetic phenomenon, by improving the drug flux, extending therapeutic potential, and extending the ability to deliver a broadened range of molecules such as peptides, hormones, and even vaccines. This review summarizes the existing evidence and points at the translational prospects of the above-mentioned technologies, as well as the future directions of clinical application and improvement of formulation in trans-dermal therapies.

Non-steroidal anti-inflammatory drugs (NSAIDs) have wide applicability in management of inflammatory and pain related diseases but limited applicability is characterized by common use and gastrointestinal disturbance. Present study is the trying to come up with sustained release (SR) matrix tablets of NSAIDs using hydrophilic and hydrophobic polymers and correlate the results of in-vitro drug release with the in-vivo pharmacokinetics response. The Ibuprofen drug was selected to be the model, and the direct compression of matrix tablet with HPMC K100M and ethyl cellulose was done. The drug was undergone in-vitro dissolution study using USP-II apparatus with phosphate buffer (pH7.2) and during in-vivo pharmacokinetics testing using healthy volunteers approach crossover study. They came up with a favourable Level An in-vitro/ in-vivo correlation (IVIVC) (R 2= 0.987), showing that the in-vitro kinetics of drug released is a fair representation of the average put on plasma. Sustained release matrix has succeeded in prolonging the duration of drug release to 12 hours and reduced Cmax which contributed to reduction of adverse effects related to a peak. These findings encourage studies into establishing the means of developing SR NSAID formulation to assist in GI toxicity and compliance in patients.