Schizophrenia Treatment Based on Sustained Release of Risperidone from Poly(lactic-co-glycolic) Acid Implantable Microarray Patch

Le résumé fourni par la source

High Resolution Image Download MS PowerPoint Slide Schizophrenia is one of the most severe mental disorders, affecting approximately 24 million people worldwide. Conventional treatments, such as drug-loaded implants and intramuscular injections, have several limitations, including pain during administration and the need for medical professionals to perform the procedure. In this study, a poly(lactic- co -glycolic) acid (PLGA)-based implantable microneedle patch (IMN) was developed for the transdermal delivery of risperidone (RIS) as a treatment for schizophrenia. RIS IMNs were prepared by sequentially casting gel-based formulations into microneedle (MN) molds. The patches were then characterized using microscopy, differential scanning calorimetry, and infrared spectroscopy, as well as through evaluations of MN insertion and RIS release. A selected formulation was further tested by evaluating its cytocompatibility and its ability to deliver RIS in a rat animal model. The RIS IMN demonstrated excellent mechanical properties, successfully inserting up to 378 nm into model skin, which is crucial for effective transdermal drug delivery. A biocompatibility study using human dermal fibroblasts showed no cytotoxicity, with cell viability and proliferation being close to 100%. The optimized formulation achieved a sustained in vitro release over 7 days, while ex vivo skin deposition and permeation studies showed over 65% RIS delivery efficiency. In vivo animal studies confirmed that RIS IMNs maintained therapeutic plasma concentrations throughout the nine-day experiment, with C max values of RIS and 9-OH RIS reaching 387.96 ± 194.02 and 139.89 ± 47.68 ng/mL at 6 and 96 h, respectively. In contrast, intramuscular injection showed a C max of 1756.70 ± 246.06 and 1377.38 ± 160.78 ng/mL at 2 and 6 h but lost therapeutic effect after just 24 h. These findings suggest that RIS IMNs offer significant clinical benefits for patients with schizophrenia, providing prolonged therapeutic effects with a simple, self-administering drug delivery system, reducing the need for frequent medical interventions.

Ce résumé expose les affirmations des auteurs. BNTIC ne l’interprète pas comme une validation indépendante des résultats.