Taste masking of water‐soluble drug by solid lipid microspheres: a child‐friendly system established by reversed lipid‐based nanoparticle technique

摘要

Abstract Objectives A child‐friendly taste‐masking strategy using solid lipid microsphere (SLM) has been proposed to obscure the undesirable taste of some water‐soluble drugs. In this study, the reversed lipid‐based nanoparticle (RLBN) technique was used to encapsulate a water‐soluble drug to facilitate the preparation of SLM. Methods The model drug used was atomoxetine hydrochloride (ATX), and a three‐step method was used to prepare ATX‐RLBN. Taste‐masking microsphere (ATX‐RLBN‐SLM) was prepared by the spray chilling method. The drug release mechanism was studied by high‐performance liquid chromatography and scanning electron microscopy. Moreover, in vitro taste evaluation method was established and ATX bioavailability was investigated employing pharmacokinetic studies. Key findings The obtained ATX‐RLBN‐SLM had smooth spherical particles with a size of about 80?μm. The drug encapsulation and loading efficiencies were 98.28%?±?0.59% and 0.89%?±?0.04%, respectively. In vitro drug release studies showed that nearly 96% drug was retained in the microspheres within 10?min at pH 6.8 and a complete release was triggered by lipase, accompanied by variation in the morphology. Taste assessment revealed that ATX‐RLBN‐SLM could efficiently mask the bitter taste and improved the bioavailability of ATX. Conclusions Atomoxetine hydrochloride‐reversed lipid‐based nanoparticle‐solid lipid microsphere exhibited excellent taste‐masking effect with negligible leakage in the oral cavity environment and thorough collapse upon lipase stimulation, simultaneously enhancing the bioavailability of ATX. The study paves a new way to efficiently mask the undesirable taste of some water‐soluble drugs.