title: Boswellia carterii liquisolid systems with promoted anti-inflammatory activity.
abstract: Boswellia carterii(BC) Birdwood oleogum resin is an ancient remedy of inflammation processes known since Ancient Egyptian time. Of boswellic acids, 3-acetyl-11-keto-β-boswellic acid (AKBA) is the most potent anti-inflammatory active principle. Liquisolid systems of the biologically active fraction of BC oleogum resin were prepared for improving dissolution properties using low dose oral delivery to achieve enhanced anti-inflammatory activity, in comparison with the standard oral anti-inflammatory; Indomethacin. AKBA was assayed, employing an accurate and sensitive HPLC method. Detection was carried out at 210 nm using UV/Vis detector. A solubility study for the bioactive fraction was conducted. Microcrystalline cellulose and Aeroperl®300 Pharma were used as carrier and coating materials. Angle of slide, liquid load factor and Carr's flow index were estimated. Six systems were prepared using polyethylene glycol 400, solvent and two drug loading concentrations; 20 and 40 %. For each concentration, three carrier: coat ratios were dispensed; 20:1, 10:1, and 5:1. Dissolution study was performed and two systems were selected for characterization and in vivo evaluation by investigating upper GIT ulcerogenic effect and anti-inflammatory efficacy in rats. Results indicate absence of ulcers and significantly higher and prolonged anti-inflammatory efficacy for formulations F1 and F2, with carrier: coat ratio, 5:1 and drug loads of 20 and 40 %, respectively, compared with standard oral indomethacin. We conclude higher efficacy of BC bioactive fraction liquisolids compared with Indomethacin with greater safety on GIT, longer duration of action and hence better patient compliance.
authors.forename: Dina Mahmoud
authors.initials: DM
authors.lastname: Mostafa
authors.forename: Nagwa Mohammed
authors.initials: NM
authors.lastname: Ammar
authors.affiliation: Department of Pharmaceutical Technology, National Research Centre, El Buhouth Street, Dokki, Giza 12622, Egypt. samehhosam@yahoo.com.
authors.forename: Sameh Hosam
authors.initials: SH
authors.lastname: Abd El-Alim
authors.forename: Ahmed Alaa
authors.initials: AA
authors.lastname: Kassem
authors.forename: Rehab Ali
authors.initials: RA
authors.lastname: Hussein
authors.forename: Gamal
authors.initials: G
authors.lastname: Awad
authors.forename: Sally Abdul-Wanees
authors.initials: SA
authors.lastname: El-Awdan
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D029743:Boswellia / Q000737:chemistry; D002351:Carrageenan; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004195:Disease Models, Animal; D004337:Drug Carriers; D005260:Female; D007213:Indomethacin / Q000494:pharmacology; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control*; D008855:Microscopy, Electron, Scanning; D008517:Phytotherapy; D010946:Plants, Medicinal; D011092:Polyethylene Glycols / Q000737:chemistry; D017208:Rats, Wistar; D012116:Resins, Plant / Q000008:administration & dosage / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D013276:Stomach Ulcer / Q000139:chemically induced; D014315:Triterpenes / Q000008:administration & dosage / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D012116:Resins, Plant; D012997:Solvents; D014315:Triterpenes; C094432:acetyl-11-ketoboswellic acid; D011092:Polyethylene Glycols; D002351:Carrageenan; D002482:Cellulose; C109691:microcrystalline cellulose; D007213:Indomethacin