Formulation development and evaluation of gastroretentive floating beads with Brucea javanica oil using ionotropic gelation technology.
10.1016/S1875-5364(18)30059-1
- Author:
Yue ZHANG
1
,
2
;
Xi-Tong ZHANG
1
,
2
;
Qi ZHANG
1
,
2
;
Bing WANG
1
,
3
;
Tong ZHANG
1
,
4
Author Information
1. Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
2. School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
3. School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address: annabel_cn@163.com.
4. School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address: zhangtdmj@hotmail.com.
- Publication Type:Journal Article
- Keywords:
Alginate–carrageenan beads;
Box–Behnken design;
Brucea javanica oil;
Gastric retention;
SPET/CT;
Simaroubaceae
- MeSH:
Alginates;
chemistry;
Animals;
Biological Availability;
Brucea;
chemistry;
Carrageenan;
chemistry;
Delayed-Action Preparations;
administration & dosage;
chemistry;
pharmacokinetics;
Drug Carriers;
chemistry;
Drug Delivery Systems;
methods;
Drug Evaluation, Preclinical;
Gastric Mucosa;
metabolism;
Glucuronic Acid;
chemistry;
Hexuronic Acids;
chemistry;
Microspheres;
Plant Oils;
administration & dosage;
chemistry;
pharmacokinetics;
Rats;
Rats, Sprague-Dawley
- From:
Chinese Journal of Natural Medicines (English Ed.)
2018;16(4):293-301
- CountryChina
- Language:English
-
Abstract:
In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box-Behnken design consisted of 1.7% alginate (W/V), 1.02% carrageenan (W/V), 1.4% CaCO (W/V), and a gelling bath of pH 0.8. The alginate-carrageenan-Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%-55% and an encapsulation efficiency of 70%-80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention (> 60% at 6 h) in fasted rats, compared to non-floating beads (15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography (SPET/CT). In conclusion, the alginate-carrageenan-Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.
