Electrospraying is renowned for its simplicity and versatility, and which can effectively produce particles with well-controlled size, size distribution, particle shape, morphology and microstructure at the nano/microscale. In this study, coaxial electrospraying was used to investigate its feasibility for preparing nanoparticles made up of nanocrystals encapsulated within a polymer shell. Firstly, aqueous nanosuspensions of darunavir were prepared by wet media milling. Then the nanosuspension and solutions of an enteric polymer, Eudragit L100, were used as the inner/core liquid and outer/shell liquid in a coaxial electorspraying setup, respectively. As long as a sufficiently high voltage was applied, a stable Taylor cone-jet mode was obtained to produce very fine core-shell structure nanoparticles with high darunavir encapsulation efficiency of approximately 90%. The influence of the starting nanosuspension and the flow rates on the characteristics of the final electrosprayed particles was also evaluated. Using an optimized nanosuspension with reasonable size, size distribution and flow rates, the enteric coating layer reduced the percentage of DRV release in acidic medium in the in vitro dissolution test to c.a. 20%. This study indicates that coaxial electrospraying is a potential and unique technique for encapsulating drug nanocrystals within a polymeric Shell.
Inflammatory bowel disease (IBD) is an idiopathic, relapsing disease involving chronic inflammation of the digestive tract, either in part or entire. IBD primarily includes Crohn’s disease (CD) and ulcerative colitis (UC) with a high prevalence rate in the industrialized world, with North America noting the highest frequency of people suffering with CD [1]. Incidence of IBD is from 31 to 71 per100,000 people for CD and 18-31 per 100,000 for UC and is increasing at an alarming rate. Although, adults are the most frequently diagnosed ones, reports show a significant population of paediatric is also being diagnosed with IBD [2].
Context: Considering that bitter taste of drugs incorporated in orally disintegrating tablets (ODTs) can be the main reason for avoiding drug therapy, it is of the utmost importance to achieve successful taste-masking. The evaluation of taste-masking effectiveness is still a major challenge.