Abstract
Polymeric nanoparticle of Doxylamine and formulated as bi- layer of dissolved microneedle transdermal dosage form
Abstract
Background: Doxylamine succinate (DS) is a first-generation antihistamine commonly use during pregnancy. Dissolving Microneedles are microscopic polymer-based needles that painlessly deliver drugs through the dermis by dissolving after insertion, offering a minimally invasive drug administration, avoiding oral route. used as a safe and effective first-line treatment for nausea and vomiting.
Aim: Preparation of bilayer microneedle of DS from biodegradable polymers; fast dissolving microneedle tips and sustained release microneedle body.
Methods: The fast-dissolving tips were formulated using a combination of 10% w /w (PVA: PVP 3:7) and cast in the microneedle silicon templet molds by using the drug as a freely soluble salt (Doxylamine succinate) by using casting method
The second layer was prepared by solvent antisolvent method to prepare a sustained release of drug as a doxylamine free base; either (an aqueous DS solution) added dropwise to, PLGA dispersed in ethyl acetate or (ethanolic solution of DS) was added dropwise to HPMC K4 dispersed in water then casted over the first layer after drying by vacuum pumps with desiccator and silica gel.
Results: The first layer of the microneedle showed fast release at the first 15 min when measured by dissolution USP-5 apparatus. The second layer showed a biphasic release extended over more than 3 days with (62 nm with 0.002 PDI) and other characterization was still under the study.
Conclusions: The dissolving polymeric microneedle transdermal dosage form can be used successfully and can be scaled up and are reproducible.
