WITHDRAWN: Biodegradable Self-assembled polymeric Micelles based on Poly (ethylene oxide)-block-Polylactide block copolymer for sustained delivery of dapsone

Abstract

Dapsone is the simplest antibiotic of sulphones that demonstrates its viability against various species of bacteria and protozoa. By restricting dihydrofolic acid synthesis through competition with para-amino benzoate, dapsone inhibits the growth of these microorganisms. Owing to its low aqueous solubility and non-specific distribution in the body, the applicability of dapsone is impeded. A control on pharmacokinetics and targeted delivery of drugs is deeply needed in order to reduce the side effects of the drug and make treatment more progressive. The aim of this study is to increase the bioavailability and efficacy of dapsone through the delivery of MeO-PEO 5K -b-PLA micelles. The effect of the length of the hydrophobic block (PLA) on micelles size, critical micelle concentration, entrapment efficiency, and release study is assessed. The PMs were prepared using the solvent evaporation process. The CMC of synthesized block copolymer was measured using a fluorescence-based method. The size and morphology of PMs was determined by dynamic light scattering (DLS) and atomic force microscopy (AFM). The entrapment efficiency and release kinetic behavior of MeO-PEO 5K -b-PLA based PMs were determined by UV-visible spectroscopy and dispersion method, respectively. The size of micelles increased and the rate of drug release decreased as the length of the PLA block increased. With copolymers having greater PLA block length, the maximum encapsulation efficiency of 89.58 percent for dapsone is attained. A comparison of dapsone's antibacterial activity against S. Aureus is performed and delivered by PMs. In comparison to pure drugs, the MIC for PMs loaded with dapsone has decreased. Morphological analysis based on AFM also verified the decrease in MIC.