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The preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system.
Pharm Dev Technol. 2020 Dec; 25(10):1226-1237.PD

Abstract

ABSTRCT Felodipine has been widely used as a poorly water-soluble model drug for various studies to improve its oral bioavailability and in vivo efficacy. In this study, we developed amorphous solid dispersions (ASDs) via spray drying to enhance the bioavailability of felodipine through using natural zein protein as a novel polymeric excipient. The solid state characterization results demonstrated a single glass transition temperature (Tg) around 128.6 °C and good physical stability post 3 months accelerated study under the condition of 40 °C and 75% relative humidity (RH), which is possibly accounted for the molecular immobilization and hydrogen bonding interactions between felodipine and zein. By combining the in vitro dissolution study with TIM-1 gastrointestinal simulation investigation, it is indicated that felodipine was rapidly released from the ASD in 30 mins, and the supersaturation of felodipine was well maintained over 6 h, which resulted in a significant enhancement of felodipine bioavailability during simulated digestive processes in the upper GI tract. This study suggests that spray drying combined with natural excipient zein is an efficient formulation strategy for the development of ASDs with enhanced aqueous solubility and bioavailability.

Authors+Show Affiliations

Department of Food Science, Rutgers, The State University of New Jersey, New Brunswick, NJ, USA. Zhejiang Hisun Pharmaceutical Co. Ltd, Hangzhou, China.Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA.Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32787680

Citation

Zhang, Hongwei, et al. "The Preparation of Felodipine/zein Amorphous Solid Dispersions and in Vitro Evaluation Using a Dynamic Gastrointestinal System." Pharmaceutical Development and Technology, vol. 25, no. 10, 2020, pp. 1226-1237.
Zhang H, Liu X, Ma X. The preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system. Pharm Dev Technol. 2020;25(10):1226-1237.
Zhang, H., Liu, X., & Ma, X. (2020). The preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system. Pharmaceutical Development and Technology, 25(10), 1226-1237. https://doi.org/10.1080/10837450.2020.1809456
Zhang H, Liu X, Ma X. The Preparation of Felodipine/zein Amorphous Solid Dispersions and in Vitro Evaluation Using a Dynamic Gastrointestinal System. Pharm Dev Technol. 2020;25(10):1226-1237. PubMed PMID: 32787680.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The preparation of felodipine/zein amorphous solid dispersions and in vitro evaluation using a dynamic gastrointestinal system. AU - Zhang,Hongwei, AU - Liu,Xu, AU - Ma,Xiangyu, Y1 - 2020/08/20/ PY - 2020/8/14/pubmed PY - 2021/7/30/medline PY - 2020/8/14/entrez KW - TIM-1 model KW - Zein KW - amorphous solid dispersions KW - bioavailability KW - solid-state characterization KW - spray drying SP - 1226 EP - 1237 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 25 IS - 10 N2 - ABSTRCT Felodipine has been widely used as a poorly water-soluble model drug for various studies to improve its oral bioavailability and in vivo efficacy. In this study, we developed amorphous solid dispersions (ASDs) via spray drying to enhance the bioavailability of felodipine through using natural zein protein as a novel polymeric excipient. The solid state characterization results demonstrated a single glass transition temperature (Tg) around 128.6 °C and good physical stability post 3 months accelerated study under the condition of 40 °C and 75% relative humidity (RH), which is possibly accounted for the molecular immobilization and hydrogen bonding interactions between felodipine and zein. By combining the in vitro dissolution study with TIM-1 gastrointestinal simulation investigation, it is indicated that felodipine was rapidly released from the ASD in 30 mins, and the supersaturation of felodipine was well maintained over 6 h, which resulted in a significant enhancement of felodipine bioavailability during simulated digestive processes in the upper GI tract. This study suggests that spray drying combined with natural excipient zein is an efficient formulation strategy for the development of ASDs with enhanced aqueous solubility and bioavailability. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/32787680/The_preparation_of_felodipine/zein_amorphous_solid_dispersions_and_in_vitro_evaluation_using_a_dynamic_gastrointestinal_system_ L2 - https://www.tandfonline.com/doi/full/10.1080/10837450.2020.1809456 DB - PRIME DP - Unbound Medicine ER -