Formulation And Characterization Of Palm Oil Esters Based Nano-Cream For Topical Delivery Of Piroxicam: Study Of In Vitro Release And In Vivo Anti-Inflammatory And Analgesic Effects
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Date
2010-06
Authors
Muthanna F. Abdulkarim
Journal Title
Journal ISSN
Volume Title
Publisher
Universiti Sains Malaysia
Abstract
During recent years, there has been increased interest in the use of topical vehicle
systems that could assist drug permeation through the skin. The drugs of interest usually
those causing or having problems when given orally, e.g., easily hydrolyzed in the
gastro-intestinal tract, poor bioavailability or to cause adverse reactions. One such drug
is piroxicam, a highly effective anti-inflammatory, anti-pyretic and analgesic but causes
gastro-intestinal ulcers and bleeding. One of the most promising vehicle systems for
trans-dermal permeation of drugs is a nano-cream, a semisolid emulsion with droplet
size of 20-200 nm. The main purpose of this study is to formulate a novel nano-cream
I
containing piroxicam for topical delivery and to use palm oil esters (POEs) a new
derrivetised palm oil as the oil phase. In the initial study, pseudotemary phase diagrams
of water, POEs and non-ionic surfactant mixture of several HLB values were
constructed and several promising nano-cream formulae were selected. The stability
under different temperatures and other properties of the formulations including the
rheological behaviour, zeta potential, droplet size and structural characteristics of the
formulation and Solubility and partition coeffecient of piroxicam were studied.
Based en the initial studies conducted on selected several tornllllae, a fonnula with
25:37:38 basic composition of palm oii esters: aqueous phase: surfactant mixture (80%
Tween 80: 20% Span 20 HLB 13. 72) was used to prepare several nano-creams using
phosphate buffer pH 4, pH 6 and pH 7.4 respectively as the external phase. The abilities
of these formulae to deliver piroxicam through cellulose acetate membrane and full
thickness rat skin were assessed in vitro using Frantz diffusion cell. E 15 and E 16 were
identified as the promising formulae and their pharmacodynamic effects were evaluated
and compared with a preparation available in market. Anti- inflammatory effect was
measured by using carragennan-induced hind paw edema method where the edema
volume was measured in term of paw thickness. The analgesic activity was measured as
the pain threshold response. In conclusion, the 0.5% nano-creams formulated by using
the POEs as the oil phase and phosphate buffer pH 6 and 7.4 as external phase were
found to have suitable rheological, droplet size and stability properties. Nano-cream (pH
7.4) E 16 had shown a better in vitro transfer through cellulose acetate membrane and
full thickness rat skin as compared to nano-cream (pH 6) and a product available in
market. This could be due to the higher flux calculated. The E 16 nano-cream (pH 7.4)
showed the best anti-inflammatory and analgesic activities among the preparations
tested.
Description
Keywords
Formulate a novel nano-cream I containing piroxicam , use palm oil esters.