Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2022 , Vol 26 , Issue 2
Preparation and optimization of berberine phospholipid complexes using QbD approach and in vivo evaluation for anti-inflammatory, analgesic and antipyretic activity
Ayça GÜNGÖR-AK1,Esra KÜPELİ-AKKOL2,Buket AKSU3,Ayşegül KARATAŞ4
1Department of Pharmaceutical Technology, Faculty of Pharmacy, ZonguldakBülent Ecevit University, Zonguldak, Turkey
2Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, Ankara, Turkey
3Department of Pharmaceutical Technology, Faculty of Pharmacy, Altinbas University, Istanbul, Turkey
4Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, Ankara, Turkey
DOI : 10.29228/jrp.135 Berberine (BER) is a benzylisoquinoline alkaloid found in many plants. It has high water solubilitybut its bioavailability is low in oral administration due to the first-pass effect in the liver and intestine. Phytosomesare are prepared by complexing herbal active ingredients and phospholipids (PLs). The aim of this study is to prepare BERphospholipidcomplexes (BPCs) using the reverse phase evaporation method. In the preparation of the formulations, the effects of BER:PL ratio (w/w), reaction temperature (°C) and reaction time (h) on the specifications of the complexes such as particle size (PS), zeta potential (ZP) and encapsulation efficiency (EE%) were investigated. The distribution of PS of obtained complexes was ranging between 339 -1259 nm and their ZP were within -4,27- -5,15 mV. The drug EE% was relatively high. Quality by Design (QbD) methods have been used in the formulation design and selection of the optimum formulation. BPCs anti-inflammatory, analgesic and antipyretic activities are evaluated by using in vivo methods.Carrageenan-, Prostaglandin E2 (PGE2)- and serotonin-induced hind paw edema, acetic acid-induced increase in capillary permeability and subcutaneous air-pouch models for the anti-inflammatory activity, inhibition of pbenzoquinone- induced abdominal constriction and hot plate test for the analgesic activity, Freund’s complete adjuvantinduced pyrexia model for the antipyretic activity were used in mice and rats. Results showed that BPCs showed potent anti-inflammatory, analgesic and antipyretic activities at the dose of 209 mg/kg. Keywords : Berberine;phytosomes; analgesic; anti-inflammatory; qbd approach
Marmara University