BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment

被引:51
作者
Ameeduzzafar [1 ]
Qumber, Mohd [2 ]
Alruwaili, Nabil K. [1 ]
Bukhari, Syed Nasir Abbas [3 ]
Alharbi, Khalid Saad [4 ]
Imam, Syed Sarim [5 ]
Afzal, Muhammad [4 ]
Alsuwayt, Bader [6 ]
Mujtaba, Ali [7 ]
Ali, Asgar [2 ]
机构
[1] Jouf Univ, Coll Pharm, Dept Pharmaceut, Aljouf, Saudi Arabia
[2] Jamia Hamdard, Sch Pharmaceut Educ & Res, Dept Pharmaceut, New Delhi, India
[3] Jouf Univ, Coll Pharm, Dept Pharmaceut Chem, Aljouf, Saudi Arabia
[4] Jouf Univ, Coll Pharm, Dept Pharmacol, Aljouf, Saudi Arabia
[5] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh, Saudi Arabia
[6] Northern Border Univ, Coll Pharm, Dept Pharmacol, Rafha, Saudi Arabia
[7] Northern Border Univ, Coll Pharm, Dept Pharmaceut, Rafha, Saudi Arabia
关键词
Itraconazole; Nanolipid carrier; Skin permeation; Skin irritation study; Antimicrobial activity; TRANSDERMAL APPLICATION; EXPERIMENTAL-DESIGN; DRUG-RELEASE; FORMULATION; NANOPARTICLES; NLC; OPTIMIZATION; VEHICLES; SODIUM; SKIN;
D O I
10.1007/s12247-019-09420-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Objectives The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R-1), entrapment efficiency (R-2), and drug release in 12 h (R-3). Results The optimized formulation ITZLNLCopt showed particle size (147.31 +/- 1.43 nm) high entrapment efficiency (86.36 +/- 0.83%) and drug release (77.23 +/- 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 +/- 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition (P< 0.05) than control gel (ITZL gel) againstCandida albicansandAspergillus fumigatus. Conclusions It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.
引用
收藏
页码:85 / 98
页数:14
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