Intravaginal mucoadhesive microspheres of tenofovir disoproxil fumarate (TDF) has been formulated using chitosan as the matrix-forming mucoadhesive polymer and evaluated. Ionotropic gelation method was used to produce the microspheres. Drug-polymer compatibility, percentage yield, particle size determination by optical microscopy, drug content & encapsulation efficiency, ex vivo mucoadhesion and in vitro release were evaluated. Based on the evaluation studies, F6 was selected as the best formulation and evaluated further for release kinetics and curve fitting analysis. F6 followed Korsmeyer-Peppas and Higuchi models. Accelerated stability study was conducted as per ICH guidelines. Drug content analysis, FTIR, XRD, SEM analysis showed that it remained stable for a period of six months.
C1 was selected as the best formulation due to better swelling index (65.93% at 24 h), prolonged release of 100.62% cumulative drug release (CDR) at 24 h, superior mucoadhesion force (35.93 × 10 dynes/cm) and retention time (16 h). The study revealed that C1 remained stable for six months. C1 showed nil systemic absorption which is desirable and according to histopathological study, C1, exhibited minimal damage on the rat vaginal epithelium indicating safety.
Sublingual tablets Purpose: Sublingual drug delivery can be an alternative and better route when compared to oral drug delivery as sublingually administered dosage forms bypass hepatic metabolism. A rapid onset of pharmacological effect is often desired for some drugs, especially those used in the treatment of acute disorders. Sublingual tablets disintegrate rapidly and the small amount of saliva present is usually sufficient for achieving disintegration of the dosage form coupled with better dissolution and increased bioavailability. Approach: Published articles from PubMed and other standard sources were utilized to review and compile an overview of sublingual tablets and the benefits of the sublingual route of administration. Findings: Sublingual tablets were found to have better characteristics when compared to conventional dosage forms. Sublingually administered tablets achieved better bioavailability, rapid onset of action and better dissolution properties due to fast disintegration. The addition of super-disintegrants facilitated rapid disintegration and this approach can be used to treat acute disorders or emergency conditions. Conclusion: Sublingual tablets or any sublingual dosage form can be used to achieve a rapid onset of action, better patient compliance and increased bioavailability. The sublingual route of administration can be used for drugs which undergo extensive first pass metabolism or degradation in the GIT. Drugs administered sublingually tend to have better bioavailability which correlates to dose reduction when compared to conventional oral tablets.
The management of nail psoriasis is an arduous task owing to the disease manifestations and anatomical structure of the nail plate. Although various treatment therapies are available for nail psoriasis, topical therapy is contemplated as one of the most favorable options as systemic therapies are accompanied by numerous side effects that result in patient incompliance. The topical formulations including creams, gels, ointments, and nail lacquers have been used as delivery systems for various antipsoriatic drugs. Among these, nail lacquers emerge to be promising and patient friendly formulations. However, the major defiance with topical delivery is inefficacious penetration of drug through impenetrable keratinized nail plate to reach the target sites: nail matrix and nail bed. Therefore, in order to obtain effectual drug delivery systems that can retain/remain on the nail plate for a prolonged period of time and deliver the drug across it, systematic approaches like quality by design (QbD) need to be followed so that the desired quality can be “built in” the system rather than to rely solely on retrograde evaluation. Furthermore, more advances in research are still required to develop a validated animal model so as to determine the efficacy of the formulation and to establish a mathematical model that can help in predicting the desirable attributes of the formulation and permeation of various molecules through the nail plate.
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