NDLI: Topical liquid crystalline gel containing lornoxicam/cyclodextrin complex

Content Provider	Springer Nature Link
Author	Ammar, H. O. Ghorab, M. Mahmoud, A. A. Makram, T. S. shi, S. H.
Copyright Year	2011
Abstract	Lornoxicam is a potent analgesic non-steroidal anti-inflammatory drug that can be used topically to relieve pain and to reduce inflammation. The objectives of this study were to improve the therapeutic efficacy of lornoxicam by complexation with cyclodextrins and to formulate it in liquid crystalline gel. Lornoxicam and β-cyclodextrin (βCD) or hydroxypropyl-β-cyclodextrin (HPβCD) complexes were prepared using the kneaded method in 1:1, 1:2, 1:3 and 1:4 drug:CD molar ratios. Inclusion complexation in aqueous solution and solid state was evaluated by the ultraviolet, phase solubility diagram, differential scanning calorimetry, X-ray diffractometry and Fourier-transform infrared spectroscopy. The stoichiometry for the inclusion complex was found to be 1:2 drug:CD molar ratio as determined from Job’s plot. This result was confirmed by the in vitro dissolution studies for the prepared complexes. Among all the prepared complexes, the complex prepared with βCD in 1:2 drug:CD molar ratio showed highest improvement in drug dissolution and was chosen to be formulated in a topical preparation. For developing liquid crystalline gel, different ratios of Brij 97, glycerol and oils (liquid paraffin, isopropyl myristate and Miglyol$^{®}$ 812) were prepared. The formula composed of Brij 97 and glycerol in 3:1 weight ratio, 10% Miglyol$^{®}$ 812 and 40% water showed higher drug release compared to the other prepared gels. Moreover, this formula showed low ex vivo permeation on excised pigskin thus it could offer high topical effect with low systematic side effects. This formula showed superior anti-inflammatory activity when applied topically on rats’ skin after induction of burn compared to that of Feldene$^{®}$ gel.
Starting Page	161
Ending Page	175
Page Count	15
File Format	PDF
ISSN	09230750
Journal	Journal of Inclusion Phenomena and Macrocyclic Chemistry
Volume Number	73
Issue Number	1-4
e-ISSN	15731111
Language	English
Publisher	Springer Netherlands
Publisher Date	2011-10-26
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Lornoxicam Cyclodextrin Complexation Physiochemical characterization Dissolution Liquid crystalline gel Topical Burn Organic Chemistry Crystallography Food Science
Content Type	Text
Resource Type	Article
Subject	Chemistry Condensed Matter Physics Food Science

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