Transdermal microemulsions of Boswellia carterii Bird: formulation, characterization and in vivo evaluation of anti-inflammatory activity.
BACKGROUND
Boswellia species are trees (family: Bruseraceae) found in India, Northern Africa and the Middle East.


OBJECTIVE
This study aims at formulating low dose biologically active fraction from the oleogum resin of Boswellia carterii (BC) in transdermal (TD) microemulsions (MEs) to acquire promoted anti-inflammatory efficacy.


METHODS
The bioactive fraction of the oleogum resin of BC was tested for solubility in different components. The most efficient were selected for constructing phase diagrams for ME preparation. The bioactive fraction was assayed by high performance liquid chromatography for 3-acetyl-11-keto-β-boswellic acid (AKBA), at 210 nm. The bioactive fraction was incorporated in 6 MEs. ME systems were evaluated for drug content and optimized systems were tested for characterization, permeation, skin irritancy and in vivo evaluation of anti-inflammatory activity.


CONCLUSIONS
Two systems were selected; ME1 and ME4 composed of Tween 80: PEG 400 at 1:1 and 2:1 ratio, with oil content 7.78 and 17.5%, respectively. The systems showed high encapsulation efficiency >83%, small droplet size <100 nm, and suitable pH for topical application. Permeation parameters for ME1 were higher compared to ME4. Both MEs were non irritant. ME1 showed significantly higher anti-inflammatory activity versus the standard TD anti-inflammatory piroxicam.


CONCLUSIONS
Optimized TD BC MEs could be used as a safe, effective and long acting alternative to oral anti-inflammatories, providing higher and prolonged efficacy and better patient compliance.
a Pharmaceutical Technology Department .
Dina Mahmoud
DM
Mostafa
b Pharmacognosy Department .
Nagwa Mohammed
NM
Ammar
a Pharmaceutical Technology Department .
Mona
M
Basha
b Pharmacognosy Department .
Rehab Ali
RA
Hussein
c Pharmacology Department , and.
Sally
S
El Awdan
d Chemistry of Natural and Microbial Products Department , National Research Center , Cairo , Egypt.
Gamal
G
Awad
D000279:Administration, Cutaneous; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology*; D029743:Boswellia; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000737:chemistry*; D005260:Female; D005989:Glycerides / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D051379:Mice; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012116:Resins, Plant; D012869:Skin Absorption; D023422:Skin Irritancy Tests; D014315:Triterpenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; C000604724:Capmul MCM C8; D004655:Emulsions; D005989:Glycerides; D011136:Polysorbates; D012116:Resins, Plant; D014315:Triterpenes; C094432:acetyl-11-ketoboswellic acid; C440220:Labrasol; D011092:Polyethylene Glycols; C000595213:polyethylene glycol 400
Anti-inflammatory; boswellic acids; skin irritancy; skin permeation; topical application