Preparation and in vivo evaluation of piroxicam-loaded gelatin microcapsule by spray drying technique.
To develop a piroxicam-loaded gelatin microcapsule with enhanced bioavailability, a gelatin microcapsule encapsulated ethanol and piroxicam has been formulated by using gelatin as a water-soluble polymer shell. The aqueous solubility and bioavailability of piroxicam in piroxicam-loaded microcapsule in rats were then evaluated compared to piroxicam powder. The piroxicam-loaded gelatin microcapsule spherical in shape with smooth surface showed the geometric mean diameter of about 19 microm. It had the piroxicam solubility of about 1.87 mg/ml and the amount of ethanol of about 4.37 microg/mg. Furthermore, it gave significantly higher total plasma concentrations, Cmax and area under the blood concentration-time curve (AUC) of piroxicam in rats than did piroxicam powder, indicating that the drug from gelatin microcapsule could be more orally absorbed in rats. In particular, the AUC of piroxicam in gelatin microcapsule was significantly about 2 fold increased compared to piroxicam powder. This enhanced oral relative bioavailability of piroxicam in gelatin microcapsule was contributed by the marked increase in the absorption rate of piroxicam due to the improved solubility of piroxicam. Thus, the piroxicam-loaded gelatin microcapsule developed using spray-drying technique with gelatin, sodium lauryl sulfate and ethanol would be useful to deliver piroxicam in a pattern that allows fast absorption in the initial phase, leading to better absorption.
College of Pharmacy, Yeungnam University, Gyongsan, South Korea.
Ming Guan
MG
Piao
Chan-Woo
CW
Yang
Dong Xun
DX
Li
Jong Oh
JO
Kim
Ki-Young
KY
Jang
Bong Kyu
BK
Yoo
Jung Ae
JA
Kim
Jong Soo
JS
Woo
Won Seok
WS
Lyoo
Sung Soo
SS
Han
Yong-Bok
YB
Lee
Dae-Duk
DD
Kim
Chul Soon
CS
Yong
Han Gon
HG
Choi
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002214:Capsules; D003890:Desiccation; D004339:Drug Compounding; D000431:Ethanol / Q000032:analysis; D005079:Excipients; D005780:Gelatin; D008297:Male; D008855:Microscopy, Electron, Scanning; D010894:Piroxicam / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D012997:Solvents / Q000032:analysis
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D005079:Excipients; D012997:Solvents; D010894:Piroxicam; D000431:Ethanol; D005780:Gelatin