Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment.
Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment.
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液体和固体自乳化给药系统（SEDDs）作为阿奇霉素口服给药载体：优化，体外表征和稳定性评估。
DOI：
10.3390/pharmaceutics12111052
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发表时间：
2020-11-04
期刊：
影响因子：
5.4
通讯作者：
Darwis Y
中科院分区：
文献类型：
--
作者：
Abou Assi R;M Abdulbaqi I;Seok Ming T;Siok Yee C;A Wahab H;Asif SM;Darwis Y
阿奇霉素（AZM）是一种大环内酯类抗生素，用于治疗各种细菌感染。已知该药物的口服生物利用度较低（37%），这可能是由于其相对较高的分子量、低溶解度、溶出率和不完全的肠道吸收。为了克服这些缺点，开发并优化了AZM的液体(L)和固体(S)自乳化给药系统（SEDDs）。基于不同表面活性剂与助表面活性剂（Smix）比例下的药物溶解度和在不同SEDDs辅料中的乳化研究，构建了8种不同的伪三元图。在蒸馏水（DW）、0.1 mM盐酸和模拟肠液（SIF）三种稀释液中，液滴粒径(DS) < 150 nm，分散度（Đ）≤0.7，透光率(T)% >85作为选择标准。L-SEDDs （L-F1(H)）和S-SEDDs （S-F1(H)）的最终配方能够满足选择要求。这两种制剂被证明是细胞相容性的，能够打开细胞上皮紧密连接（TJ）。药物溶出度研究表明，5 min后，液体和固体SEDDs制剂中AZM的释放率分别为90%和52.22%，而纯AZM的释放率为11.27%，表明所研制的SEDDs可增强药物的口服给药能力。该配方在冷藏条件下稳定。
Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.
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DOI：
10.1016/s1387-2656(05)11004-7
发表时间：
2005-01-01
期刊：
BIOTECHNOLOGY ANNUAL REVIEW, VOL 11
影响因子：
--
作者：
Berridge, MV;Herst, PM;Tan, AS
通讯作者：
Tan, AS
影响因子：
4.9
作者：
Asgrimsson, V;Gudjonsson, T;Baldursson, O
通讯作者：
Baldursson, O
影响因子：
5.8
作者：
Buya, Aristote B.;Ucakar, Bernard;Preat, Veronique
通讯作者：
Preat, Veronique
影响因子：
5.2
作者：
Beg, Sarwar;Katare, O. P.;Singh, Bhupinder
通讯作者：
Singh, Bhupinder
影响因子：
5.5
作者：
Adeli, Ehsan;Mortazavi, Seyed Alireza
通讯作者：
Mortazavi, Seyed Alireza