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

被引:52
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
相关论文
共 43 条
[1]   Nanostructured lipid carriers of pioglitazone for transdermal application: from experimental design to bioactivity detail [J].
Alam, Sohrab ;
Aslam, Mohammed ;
Khan, Anam ;
Imam, Syed Sarim ;
Aqil, Mohammed ;
Sultana, Yasmin ;
Ali, Asgar .
DRUG DELIVERY, 2016, 23 (02) :601-609
[2]   Chitosan nanoparticles amplify the ocular hypotensive effect of cateolol in rabbits [J].
Ameeduzzafar ;
Ali, Javed ;
Bhatnagar, Aseem ;
Kumar, Neeraj ;
Ali, Asgar .
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 2014, 65 :479-491
[3]   Development and evaluation of novel itraconazole-loaded intravenous nanoparticles [J].
Chen, Wei ;
Gu, Bing ;
Wang, Hao ;
Pan, Jun ;
Lu, Weiyue ;
Hou, Huimin .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2008, 362 (1-2) :133-140
[4]  
Draize JH, 1944, J PHARMACOL EXP THER, V82, P377
[5]   New inhalation-optimized itraconazole nanoparticle-based dry powders for the treatment of invasive pulmonary aspergillosis [J].
Duret, Christophe ;
Wauthoz, Nathalie ;
Sebti, Thami ;
Vanderbist, Francis ;
Amighi, Karim .
INTERNATIONAL JOURNAL OF NANOMEDICINE, 2012, 7 :5475-5489
[6]   Formulation of LDL Targeted Nanostructured Lipid Carriers Loaded with Paclitaxel: A Detailed Study of Preparation, Freeze Drying Condition, and In Vitro Cytotoxicity [J].
Emami, Jaber ;
Rezazadeh, Mahboubeh ;
Varshosaz, Jaleh ;
Tabbakhian, Majid ;
Aslani, Abolfazl .
JOURNAL OF NANOMATERIALS, 2012, 2012
[7]   Lipid nanoparticles as vehicles for topical psoralen delivery: Solid lipid nanoparticles (SLN) versus nanostructured lipid carriers (NLC) [J].
Fang, Jia-You ;
Fang, Chia-Lang ;
Liu, Chi-Hsien ;
Su, Yu-Han .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2008, 70 (02) :633-640
[8]   Formulation and optimization of itraconazole polymeric lipid hybrid nanoparticles (Lipomer) using box behnken design [J].
Gajra, Balaram ;
Dalwadi, Chintan ;
Patel, Ravi .
DARU-JOURNAL OF PHARMACEUTICAL SCIENCES, 2015, 23
[9]   Quality by Design (QbD)-enabled development of aceclofenac loaded-nano structured lipid carriers (NLCs): An improved dermatokinetic profile for inflammatory disorder(s) [J].
Garg, Neeraj K. ;
Sharma, Gajanand ;
Singh, Bhupinder ;
Nirbhavane, Pradip ;
Tyagi, Rajeev K. ;
Shukla, Rahul ;
Katare, O. P. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2017, 517 (1-2) :413-431
[10]   Nanostructured lipid carriers for the topical delivery of tretinoin [J].
Ghate, Vivek M. ;
Lewis, Shaila A. ;
Prabhu, Prabhakara ;
Dubey, Akhilesh ;
Patel, Nilkumar .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2016, 108 :253-261