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


CONCLUSIONS
The nanocream containing the newly synthesized POEs was successful for trans-dermal delivery of piroxicam.
School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia. muthana_albuldawy@yahoo.com
Muthanna F
MF
Abdulkarim
Ghassan Z
GZ
Abdullah
Mallikarjun
M
Chitneni
Ibrahim M
IM
Salman
Omar Z
OZ
Ameer
Mun F
MF
Yam
Elrashid S
ES
Mahdi
Munavvar A
MA
Sattar
Mahiran
M
Basri
Azmin M
AM
Noor
D000287:Administration, Topical; D000700:Analgesics / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001693:Biological Transport, Active; D004951:Esterification; D066298:In Vitro Techniques; D008567:Membranes, Artificial; D050997:Nanomedicine; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry*; D017288:Pain Threshold / Q000187:drug effects; D000073878:Palm Oil; D010539:Permeability; D010894:Piroxicam / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010938:Plant Oils / Q000737:chemistry; D051381:Rats; D012867:Skin / Q000187:drug effects / Q000378:metabolism / Q000473:pathology
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D008567:Membranes, Artificial; D010938:Plant Oils; D010894:Piroxicam; D000073878:Palm Oil