Pharmaceutical Sciences and Health Technologies 4.
Stifter-Mursits, Marcell, MSc
OGN891
Department of Pharmaceutical Chemistry - Semmelweis University
+36303223023
stifter.mursits.marcell@semmelweis.hu
Cyclodextrin inclusion complexes of Boswellia serrata extract: comparative in vitro evaluation of dissolution enhancement and intestinal permeability
Marcell Stifter-Mursits1, Réka E. Angi1, Vivien Bárdos1, György T. Balogh1, Péter Püski2
1: Department of Pharmaceutical Chemistry - Semmelweis University
2: Institute of Pharmacognosy - University of Szeged
Szóbeli
Pharmaceutical Sciences and Health Technologies 4.
Hungarian
Pharmaceutical Sciences and Health Technologies
Introduction
Cyclodextrins (CDs) are cyclic oligosaccharides capable of forming inclusion complexes with lipophilic compounds, improving their solubility, permeability and pharmacokinetical performance. Boswellic acids (BAs), derived from Boswellia serrata resin, exhibit anti-inflammatory and other pharmacological activities, but are limited by extremely low aqueous solubility (less than 10 µg/mL) and poor pharmacokinetics.
Aims
Our study focused on the systematic evaluation of CD–BA interactions using complementary in vitro and ex vivo models to identify formulations capable of overcoming solubility- and permeability-related limitations.
Methods
Multiple CDs differing in cavity size and charge were screened. Selected systems were characterized by PXRD, FT-IR, and DSC. Pharmacokinetic performance was assessed using dissolution in biorelevant media, paralell artificial membrane permeation assay (PAMPA), and ex vivo permeation across porcine small intestine.
Results
The feasibility results indicated that CDs with larger cavity size and neutral charge show better interaction with BAs. The solid-state analyses confirmed the formation of inclusion complexes with the native γ-CD. The dissolution of BAs was improved over 10-fold in fasted-state media and enabled complete drug release in fed-state. The effective permeability of BAs in fasted-state was significantly higher in our PAMPA model with both γ-CD and HP-γ-CD. Ex vivo studies established γ-CD as the superior excipient with 15-fold increase in the concentration of BAs on the acceptor side.
Conclusions
Cyclodextrin selection was identified as the critical determinant of formulation performance for boswellic acids. Among the systems investigated, γ-CD consistently provided the most favorable outcomes across solid-state characterization, dissolution, and permeability studies. These findings establish native γ-CD as the optimal excipient for further development of Boswellia formulations.
Funding
The Boswellia Serrata Roxb. extracts were received from the Department of Pharmacognosy, University of Szeged, Hungary. The cyclodextrins used in the study were kind gifts of CycloLab Ltd., Budapest, Hungary.
stifter.mursits.marcell@semmelweis.hu – oral presentation
Semmelweis University – Department of Pharmaceutical Chemistry
Prof. Balogh György Tibor
Semmelweis University
György Tibor Balogh
I do not give consent to the publication of my abstract on the website of the congress.
in doctoral studies after complex exam (PhD)
Szabad
elfogadva
szóbeli
nem hagyta jóvá
9076
17:15
17:25