Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies

Abstract

Background: Dapsone is described as being active against Mycobacterium leprae, hence its role in the treatment of leprosy and related pathologies. Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance. Nanoemulsions are pharmaceutical delivery systems derived from micellar solutions with a good capacity for improving absorption. The aim of this work was to develop and compare the permeability of a series of dapsone nanoemulsions in Caco-2 cell culture against that of effective permeability in the human body simulated using Gastroplus TM software. Methods and results:The release profiles of the dapsone nanoemulsions using different combinations of surfactants and cosolvent showed a higher dissolution rate in simulated gastric and enteric fluid than did the dispersed dapsone powder. The drug release kinetics were consistent with a Higuchi model. Conclusion: This comparison of dapsone permeability in Caco-2 cells with effective permeability in the human body simulated by Gastroplus showed a good correlation and indicates potential improvement in the biodisponibility of dapsone using this new system.

Co-delivery of 5-Fluorouracil and Curcumin Nanohybrid Formulations for Improved Chemotherapy Against Oral Squamous Cell Carcinoma

“…The release pattern was pH sensitive and complemented in acidic pH that ultimately enhanced the intracellular uptake within the cancer cell which lies from 6.5 to 7.6 pH. The earlier report on NEs was stated that NE formulations have shown aggregation within drug particle, and so it reflected over the release pattern, and ultimately down-regulation of antitumor activity was reported due to large particle size [22]. 5-FU/Cur-NE/5-FU-Cur-NE formulations stability data were also collected up to 6 months, to fallow the timedependent alteration in physical appearance, phase separation, drug precipitation, entrapment efficiency and particle size, and collected data have shown satisfactory results.…”

Nanoemulsion formulations for anti-cancer agent piplartine—Characterization, toxicological, pharmacokinetics and efficacy studies

“…Nanoemulsions promote the dispersion of lipophilic drug and therefore, enhance the rate and extent of dissolution in the dissolution media (Monteiro et al, 2012; Onoue et al, 2010). In fact, for poorly water-soluble drug such as PL, the rate and extent of dissolution dictates the absorption rate from the gastrointestinal tract (Amidon et al, 1995).…”

Drug Delivery Systems on Leprosy Therapy: Moving Towards Eradication?

“…Smart pH-sensitive hydrogels can also be used to produce oral formulations. Chaves and colleagues have designed chitosan-based hydrogels for DAP oral delivery [ 74 ]. High concentrations of the drug were incorporated in the hydrogels (about 8 mg per 28 mg of formulation) and exhibited a controlled drug release under gastro-intestinal conditions.…”