[PMID]: | 27151135 |
[Au] Autor: | Wang Y; Wang S; Firempong CK; Zhang H; Wang M; Zhang Y; Zhu Y; Yu J; Xu X |
[Ad] Endereço: | Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, 212013, People's Republic of China. |
[Ti] Título: | Enhanced Solubility and Bioavailability of Naringenin via Liposomal Nanoformulation: Preparation and In Vitro and In Vivo Evaluations. |
[So] Source: | AAPS PharmSciTech;18(3):586-594, 2017 Apr. |
[Is] ISSN: | 1530-9932 |
[Cp] País de publicação: | United States |
[La] Idioma: | eng |
[Ab] Resumo: | This study was aimed at preparing orally administered naringenin-loaded liposome for pharmacokinetic and tissue distribution studies in animal models. The liposomal system, consisting of phospholipid, cholesterol, sodium cholate, and isopropyl myristate, was prepared using the thin-film hydration method. Physicochemical characterization of naringenin-loaded liposome such as particle size, zeta potential, and encapsulation efficiency produced 70.53 ± 1.71 nm, -37.4 ± 7.3 mV, and 72.2 ± 0.8%, respectively. The in vitro release profile of naringenin from the formulation in three different media (HCl solution, pH 1.2; acetate buffer solution, pH 4.5; phosphate buffer solution, pH 6.8) was significantly higher than the free drug. The in vivo studies also revealed an increase in AUC of the naringenin-loaded liposome from 16648.48 to 223754.0 ng·mL h as compared with the free naringenin. Thus, approximately 13.44-fold increase in relative bioavailability was observed in mice after oral administration. The tissue distribution further showed that the formulation was very predominant in the liver. These findings therefore indicated that the liposomal formulation significantly improved the solubility and oral bioavailability of naringenin, thus leading to wider clinical applications. |
[Mh] Termos MeSH primário: |
Flavanonas/química Flavanonas/metabolismo Lipossomos/química Nanopartículas/química
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[Mh] Termos MeSH secundário: |
Administração Oral Animais Disponibilidade Biológica Química Farmacêutica/métodos Colesterol/metabolismo Fígado/metabolismo Masculino Camundongos Tamanho da Partícula Fosfolipídeos/metabolismo Ratos Ratos Sprague-Dawley Colato de Sódio/metabolismo Solubilidade Distribuição Tecidual/efeitos dos fármacos
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[Pt] Tipo de publicação: | JOURNAL ARTICLE |
[Nm] Nome de substância:
| 0 (Flavanones); 0 (Liposomes); 0 (Phospholipids); 97C5T2UQ7J (Cholesterol); HN5425SBF2 (naringenin); NU3Y4CCH8Z (Sodium Cholate) |
[Em] Mês de entrada: | 1707 |
[Cu] Atualização por classe: | 170713 |
[Lr] Data última revisão:
| 170713 |
[Sb] Subgrupo de revista: | IM |
[Da] Data de entrada para processamento: | 160507 |
[St] Status: | MEDLINE |
[do] DOI: | 10.1208/s12249-016-0537-8 |
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