Experimental optimization of Lornoxicam liposomes for sustained topical delivery

被引:45
作者
Joshny, Joseph [1 ]
Hari, B. N. Vedha [1 ]
Devi, D. Ramya [1 ]
机构
[1] SASTRA Univ, Sch Chem & Biotechnol, Thanjavur 613401, Tamil Nadu, India
关键词
Lornoxicam; Liposomes; Central Composite Design; Thin film hydration method; TRANSFORM INFRARED-SPECTROSCOPY; IN-VITRO EVALUATION; RELEASE; DRUGS; PROLIFERATION; NANOLIPOSOMES; FORMULATION; STABILITY; MODEL; RATS;
D O I
10.1016/j.ejps.2017.10.032
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The purpose of the present investigation is to formulate liposomes of Lornoxicam for topical delivery using Central Composite Design, to provide a sustained release of the drug and thereby extend its elimination half-life. Liposomes were prepared by thin film hydration method with pH induced vesiculation. The liposomes were assessed for their particle size, charge, morphology and drug entrapment and characterized using TGA-DSC and FTIR analysis, to assess the interaction between the drug and excipients. The in vitro release study was performed using modified USP dissolution apparatus-I using three different dissolution media and the ex vivo release study was performed using goat skin. The cytotoxicity of Lornoxicam liposomes were studied on NIH 3T3 cells by MTT assay. The optimized formulation with particle size ranging from 100-200 nm provided sustained release for 8 h. The characterization studies proved very less interactions between the drug and the excipients. The ex vivo studies showed flux value of 23.29 mu g/cm(2)/h and Kp 0.011645 cm/h. The cytotoxicity study showed increase in toxicity with increase in concentration more than 0.5 mu g/mL. The in vivo skin toxicity studies and histopathology analysis showed absence of toxic lesions, which confirmed the suitability of the formulation for topical application. Lornoxicam liposomes with good skin permeation and sustained release of drug were finally optimized by the experimental design.
引用
收藏
页码:38 / 51
页数:14
相关论文
共 63 条
[1]   Standardized in vitro drug release test for colloidal drug carriers using modified USP dissolution apparatus I [J].
Abdel-Mottaleb, Mona M. A. ;
Lamprecht, Alf .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2011, 37 (02) :178-184
[2]   Liposome: classification, preparation, and applications [J].
Akbarzadeh, Abolfazl ;
Rezaei-Sadabady, Rogaie ;
Davaran, Soodabeh ;
Joo, Sang Woo ;
Zarghami, Nosratollah ;
Hanifehpour, Younes ;
Samiei, Mohammad ;
Kouhi, Mohammad ;
Nejati-Koshki, Kazem .
NANOSCALE RESEARCH LETTERS, 2013, 8
[3]   Repeated subcutaneous administrations of krokodil causes skin necrosis and internal organs toxicity in Wistar rats: putative human implications [J].
Alves, Emanuele Amorim ;
Brandao, Pedro ;
Neves, Joao Filipe ;
Cravo, Sara Manuela ;
Soares, Jose Xavier ;
Grund, Jean-Paul C. ;
Duarte, Jose Alberto ;
Afonso, Carlos M. M. ;
Pereira Netto, Annibal Duarte ;
Carvalho, Felix ;
Dinis-Oliveira, Ricardo Jorge .
HUMAN PSYCHOPHARMACOLOGY-CLINICAL AND EXPERIMENTAL, 2017, 32 (03)
[4]  
[Anonymous], 2010, OPEN CRYSTALLOGR J
[5]  
[Anonymous], 2009, Int. J. Drug Delivery Technol, DOI [10.25258/ijddt.v1i2.8839, DOI 10.25258/IJDDT.V1I1.8834]
[6]  
Atrooz O. M., 2011, International Journal of Biological Chemistry, V5, P314, DOI 10.3923/ijbc.2011.314.321
[7]  
AtulBendale R, 2011, J CHEM PHARM RES, V3, P258
[8]   Enhancement of skin permeation and anti-inflammatory effect of indomethacin using microemulsion [J].
Barakat, Nahla ;
Fouad, Ehab ;
Elmedany, Azza .
ASIAN JOURNAL OF PHARMACEUTICS, 2011, 5 (03) :141-149
[9]  
Begum M.Y., 2012, INT J PHARM TECH RES, V4, P218
[10]   Potent anti-inflammatory/analgesic effects of lornoxicam in comparison to other NSAIDS: A c-Fos study in the rat [J].
Buritova J. ;
Besson J.-M. .
InflammoPharmacology, 1997, 5 (4) :331-341