The utility of self-emulsifying oil formulation to improve the poor solubility of the anti HIV drug CSIC.
The utility of self-emulsifying oil formulation to improve the poor solubility of the anti HIV drug CSIC.
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DOI：
10.1186/1742-6405-10-14
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发表时间：
2013-05-31
影响因子：
2.2
通讯作者：
Esimone CO
中科院分区：
文献类型：
--
作者：
Obitte NC;Rohan LC;Adeyeye CM;Parniak MA;Esimone CO
CSIC （5-chloro-3-phenylsulfonylindole-2-carboxamide）是一种非核苷类逆转录酶抑制剂（NNRTI），由于其水溶性低、生物利用度差，尚未被作为治疗性抗hiv候选药物。本工作的目的是将CSIC配制成自乳化油配方，以提高其水溶性并评估其体外抗逆转录病毒活性。配制了CSIC自乳化油配方（SEFs），并对其液滴大小、zeta电位、多分散性指数（PDI）、粘度、乳化时间、稳定性和生物活性进行了评价。结果表明，CSIC在SEFs中的溶解度显著提高。助表面活性剂的浓度影响液滴的尺寸、zeta电位和多分散性指数。体外生物活性研究表明，CSIC SEFs保留了充分的抗hiv活性。首次尝试制备CSIC SEFs的体外数据表明，通过该递送系统改善CSIC的水溶性可能通过提高生物利用度来增强其体内抗逆转录病毒有效性。因此，该制剂旨在作为预防和治疗用途的口服抗hiv药物。
CSIC (5-chloro-3-phenylsulfonylindole-2-carboxamide), a non-nucleoside reverse transcriptase inhibitor (NNRTI) has not been advanced as a therapeutic anti-HIV candidate drug due to its low aqueous solubility and poor bioavailability. The objective of this work was to formulate CSIC into self-emulsifying oil formulations for the purpose of improving its aqueous solubility and evaluating in vitro antiretroviral activity. CSIC self-emulsifying oil formulations (SEFs) were formulated and evaluated for droplet size, zeta potential, polydispersity index (PDI), viscosity, emulsification time, stability and bioactivity. Results showed significantly improved solubility of CSIC in the SEFs.The concentration of co-surfactant affected the droplet size, zeta potential and polydispersity index. In vitro bioactivity studies showed that the CSIC SEFs retained full anti-HIV activity. The in vitro data from this first attempt to formulate CSIC SEFs suggest that improvement on the aqueous solubility of CSIC through this delivery system may accentuate its antiretroviral effectiveness in vivo via bioavailability enhancement. The formulation is therefore intended as an oral anti-HIV agent for prophylactic and therapeutic uses.
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影响因子：
4.9
作者：
Kasim, Nehal A.;Whitehouse, Marc;Amidon, Gordon L.
通讯作者：
Amidon, Gordon L.
影响因子：
5.8
作者：
Kommuru, TR;Gurley, B;Reddy, IK
通讯作者：
Reddy, IK
影响因子：
5.8
作者：
Khoo, SM;Humberstone, AJ;Charman, WN
通讯作者：
Charman, WN
影响因子：
3.4
作者：
Gershanik, T;Benita, S
通讯作者：
Benita, S
DOI：
10.1073/pnas.212400099
发表时间：
2002-10-15
影响因子：
11.1
作者：
Münk, C;Brandt, SM;Landau, NR
通讯作者：
Landau, NR