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The use of amphiphilic copolymer in the solid dispersion formulation of nimodipine to inhibit drug crystallization in the release media: Combining nano-drug delivery system with solid preparations.
Wei, Min-Yan; Lei, Xue-Ping; Fu, Jing-Jing; Chen, Ming-Yue; Li, Jie-Xia; Yu, Xi-Yong; Lin, Yin-Lei; Liu, Jing-Ping; Du, Ling-Ran; Li, Xin; Zhang, Yu; Miao, Ying-Ling; Huang, Yu-Gang; Liang, Lu; Fu, Ji-Jun.
Afiliação
  • Wei MY; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Lei XP; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Fu JJ; Jiangsu Provincial Xuzhou Pharmaceutical Vocational College, Xuzhou 221116, China.
  • Chen MY; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Li JX; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Yu XY; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Lin YL; School of Materials Science and Energy Engineering, Foshan University, Foshan 528000, China.
  • Liu JP; Department of Clinical Laboratory, The Third Affiliated Hospital, Southern Medical University, Guangzhou, China.
  • Du LR; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Li X; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Zhang Y; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Miao YL; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Huang YG; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Liang L; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
  • Fu JJ; The Fifth Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong 510700, China; The State Key Laboratory of Respiratory Disease, Guangzhou Medical University, Guangzhou, Guangdong, China; The Key Laboratory of Molecular Target & Clinical Pharmacol
Mater Sci Eng C Mater Biol Appl ; 111: 110836, 2020 Jun.
Article em En | MEDLINE | ID: mdl-32279765
Solid dispersion is a widely used method to improve the dissolution and oral bioavailability of water-insoluble drugs. However, due to the strong hydrophobicity, the drug crystallization in the release media after drug dissolution and the resulted decreased drug absorption retards the use of solid dispersions. It is widely known that the amphiphilic copolymer can encapsulate the hydrophobic compounds and help form stable nano-dispersions in water. Inspired by this, we tried to formulate the solid dispersion of nimodipine by using amphipathic copolymer as one of the carriers. Concerning the solid dispersions, there are many important points involved in these formulations, such as the miscibility between the drug and the carriers, the storage stability of solid dispersions, the dissolution enhancement and so on. In this study, a systemic method is proposed. In details, the supersaturation test and the glass transition temperature (Tg) measurement to predict the crystallization inhibition, the ratios of different components and the storage stability, the interactions among the components were investigated in detail by nuclear magnetic resonance (1H NMR) and isothermal titration calorimetry (ITC) and, the final dissolution and oral bioavailability enhancement. It was found that the amphiphilic copolymer used in the solid dispersion encouraged the formation the drug loading micelles in the release media and, finally, the problem of drug crystallization in the dissolution process was successfully solved.
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Texto completo: 1 Coleções: 01-internacional Temas: Geral Base de dados: MEDLINE Assunto principal: Tensoativos / Nimodipina / Sistemas de Liberação de Medicamentos / Nanopartículas / Liberação Controlada de Fármacos Limite: Animals / Humans Idioma: En Revista: Mater Sci Eng C Mater Biol Appl Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Temas: Geral Base de dados: MEDLINE Assunto principal: Tensoativos / Nimodipina / Sistemas de Liberação de Medicamentos / Nanopartículas / Liberação Controlada de Fármacos Limite: Animals / Humans Idioma: En Revista: Mater Sci Eng C Mater Biol Appl Ano de publicação: 2020 Tipo de documento: Article