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Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream.

Abdulkarim MF, Abdullah GZ, Chitneni M, Salman IM, Ameer OZ, Yam MF, Mahdi ES, Sattar MA, Basri M, Noor AM - Int J Nanomedicine (2010)

Bottom Line: The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel.Pharmacodynamically, nanocream formula F3 exhibited the highest anti- inflammatory and analgesic effects as compared with the other formulae.The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia. muthana_albuldawy@yahoo.com

ABSTRACT

Introduction: During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, anti-pyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs)-based nanocream containing piroxicam for topical delivery.

Methods: A ratio of 25:37:38 of POEs: external phase: surfactants (Tween 80:Span 20, in a ratio 80:20), respectively was selected as the basic composition for the production of a nanocream with ideal properties. Various nanocreams were prepared using phosphate-buffered saline as the external phase at three different pH values. The abilities of these formulae to deliver piroxicam were assessed in vitro using a Franz diffusion cell fitted with a cellulose acetate membrane and full thickness rat skin. These formulae were also evaluated in vivo by comparing their anti-inflammatory and analgesic activities with those of the currently marketed gel.

Results: After eight hours, nearly 100% of drug was transferred through the artificial membrane from the prepared formula F3 (phosphate-buffered saline at pH 7.4 as the external phase) and the marketed gel. The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel. Pharmacodynamically, nanocream formula F3 exhibited the highest anti- inflammatory and analgesic effects as compared with the other formulae.

Conclusion: The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam.

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Related in: MedlinePlus

Comparative mean in vitro cellulose acetate membrane transport profiles of piroxicam from formulations F2, F3 and reference gel.Note: Mean ± S.D., N = 3.
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f1-ijn-5-915: Comparative mean in vitro cellulose acetate membrane transport profiles of piroxicam from formulations F2, F3 and reference gel.Note: Mean ± S.D., N = 3.

Mentions: Drug transfer rates through the cellulose membranes of both nanocream formulae were compared with the transfer rate of the commercially available 0.5% piroxicam gel. Figure 1 shows a considerably higher and faster drug transfer rate across the membrane for nanocream F3 than for nanocream F2. It can be observed that drug transfer through the membrane is affected by the pH of the external phase of the nanocream. This difference in drug transfer may be attributed to the difference in the solubility of piroxicam at different pH conditions. Piroxicam with its weak acidic properties is more soluble in pH 7.4 buffer than in pH 6 buffer. Due to its high solubility at pH 7.4, partitioning of piroxicam from the oil phase to pH 7.4 buffer would be higher, hence leading to a higher drug transfer rate.


Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream.

Abdulkarim MF, Abdullah GZ, Chitneni M, Salman IM, Ameer OZ, Yam MF, Mahdi ES, Sattar MA, Basri M, Noor AM - Int J Nanomedicine (2010)

Comparative mean in vitro cellulose acetate membrane transport profiles of piroxicam from formulations F2, F3 and reference gel.Note: Mean ± S.D., N = 3.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2990385&req=5

f1-ijn-5-915: Comparative mean in vitro cellulose acetate membrane transport profiles of piroxicam from formulations F2, F3 and reference gel.Note: Mean ± S.D., N = 3.
Mentions: Drug transfer rates through the cellulose membranes of both nanocream formulae were compared with the transfer rate of the commercially available 0.5% piroxicam gel. Figure 1 shows a considerably higher and faster drug transfer rate across the membrane for nanocream F3 than for nanocream F2. It can be observed that drug transfer through the membrane is affected by the pH of the external phase of the nanocream. This difference in drug transfer may be attributed to the difference in the solubility of piroxicam at different pH conditions. Piroxicam with its weak acidic properties is more soluble in pH 7.4 buffer than in pH 6 buffer. Due to its high solubility at pH 7.4, partitioning of piroxicam from the oil phase to pH 7.4 buffer would be higher, hence leading to a higher drug transfer rate.

Bottom Line: The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel.Pharmacodynamically, nanocream formula F3 exhibited the highest anti- inflammatory and analgesic effects as compared with the other formulae.The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia. muthana_albuldawy@yahoo.com

ABSTRACT

Introduction: During recent years, there has been growing interest in use of topical vehicle systems to assist in drug permeation through the skin. Drugs of interest are usually those that are problematic when given orally, such as piroxicam, a highly effective anti-inflammatory, anti-pyretic, and analgesic, but with the adverse effect of causing gastrointestinal ulcers. The present study investigated the in vitro and in vivo pharmacodynamic activity of a newly synthesized palm oil esters (POEs)-based nanocream containing piroxicam for topical delivery.

Methods: A ratio of 25:37:38 of POEs: external phase: surfactants (Tween 80:Span 20, in a ratio 80:20), respectively was selected as the basic composition for the production of a nanocream with ideal properties. Various nanocreams were prepared using phosphate-buffered saline as the external phase at three different pH values. The abilities of these formulae to deliver piroxicam were assessed in vitro using a Franz diffusion cell fitted with a cellulose acetate membrane and full thickness rat skin. These formulae were also evaluated in vivo by comparing their anti-inflammatory and analgesic activities with those of the currently marketed gel.

Results: After eight hours, nearly 100% of drug was transferred through the artificial membrane from the prepared formula F3 (phosphate-buffered saline at pH 7.4 as the external phase) and the marketed gel. The steady-state flux through rat skin of all formulae tested was higher than that of the marketed gel. Pharmacodynamically, nanocream formula F3 exhibited the highest anti- inflammatory and analgesic effects as compared with the other formulae.

Conclusion: The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam.

Show MeSH
Related in: MedlinePlus