title: Microstructural investigation using synchrotron radiation X-ray microtomography reveals taste-masking mechanism of acetaminophen microspheres.
abstract: The structure of solid drug delivery systems has considerable influence on drug release behaviors from particles and granules and also impacts other properties relevant to release characteristics such as taste. In this study, lipid-based microspheres of acetaminophen were prepared to mask the undesirable taste of drug and therefore to identify the optimal formulation for drug release. Synchrotron radiation X-ray computed microtomography (SR-μCT) was used to investigate the fine structural architectures of microspheres non-destructively at different sampling times during drug release test, which were simultaneously determined to quantitatively correlate the structural data with drug release behaviors. The results demonstrated that the polymeric formulation component, namely, cationic polymethacrylate (Eudragit E100), was the key factor to mask the bitter taste of acetaminophen by inhibiting immediate drug release thereby reducing the interaction intensity of the bitter material with the oral cavity taste buds. The structure and morphology of the microspheres were found to be influenced by the shape and particle size of the drug, which was also an important factor for taste-masking performance. The quantitative analysis generated detailed structural information which was correlated well with drug release behaviors. Thus, SR-μCT has been proved as a powerful tool to investigate the fine microstructure of particles and provides a new approach in the design of particles for taste masking.
authors.affiliation: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Institute of Cancer Therapeutics, School of Life Sciences, University of Bradford, Bradford, West Yorkshire BD7 1DP, United Kingdom.
authors.forename: Zhen
authors.initials: Z
authors.lastname: Guo
authors.affiliation: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Bradford, Bradford, West Yorkshire BD7 1DP, United Kingdom.
authors.forename: Xianzhen
authors.initials: X
authors.lastname: Yin
authors.affiliation: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Key Laboratory of Modern Preparation Chinese Materia Medica of Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
authors.forename: Congbiao
authors.initials: C
authors.lastname: Liu
authors.affiliation: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Li
authors.initials: L
authors.lastname: Wu
authors.affiliation: Key Laboratory of Modern Preparation Chinese Materia Medica of Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
authors.forename: Weifeng
authors.initials: W
authors.lastname: Zhu
authors.affiliation: University of Bradford, Bradford, West Yorkshire BD7 1DP, United Kingdom.
authors.forename: Qun
authors.initials: Q
authors.lastname: Shao
authors.affiliation: University of Bradford, Bradford, West Yorkshire BD7 1DP, United Kingdom. Electronic address: p.york@bradford.ac.uk.
authors.forename: Peter
authors.initials: P
authors.lastname: York
authors.affiliation: Institute of Cancer Therapeutics, School of Life Sciences, University of Bradford, Bradford, West Yorkshire BD7 1DP, United Kingdom. Electronic address: l.h.patterson@bradford.ac.uk.
authors.forename: Laurence
authors.initials: L
authors.lastname: Patterson
authors.affiliation: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Key Laboratory of Modern Preparation Chinese Materia Medica of Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China. Electronic address: jwzhang@simm.ac.cn.
authors.forename: Jiwen
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000082:Acetaminophen / Q000008:administration & dosage* / Q000737:chemistry; D000179:Acrylates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D065546:Drug Liberation; D008055:Lipids / Q000737:chemistry; D008863:Microspheres; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D017356:Synchrotrons; D013649:Taste; D055114:X-Ray Microtomography / Q000379:methods
chemical_list: D000179:Acrylates; C477020:Eudragit E100; D008055:Lipids; D011108:Polymers; D000082:Acetaminophen
keywords: Dissolution test; Lipid microspheres; Microstructure; Synchrotron radiation X-ray computed microtomography; Taste masking; Three dimensional reconstruction