Development of novel gastroretentive salbutamol sulfate-loaded sodium alginate-pectin bubble beads prepared by co-axial needle air-injection method and in vivo clinical evaluation by ultrasound studies.
Eur J Pharm Sci
; 122: 359-373, 2018 Sep 15.
Article
in En
| MEDLINE
| ID: mdl-30017846
ABSTRACT
In the present study, the salbutamol sulfate-loaded sodium alginate-pectin (SS-loaded SA-PEC) bubble beads have been optimized and evaluated for drug loading, in vitro drug release, in vivo floating behavior in the stomach, etc. Nine batches (F1-F9) of bubble beads with different SA and PEC contents were prepared by novel co-axial needle air-injection method and related to their percent drug loading efficiency (%DLE) and percent drug release at 4â¯h (%R4h) as response factors. The multivariate analysis has shown the effect of SA/PEC ratio, total polymer content, as well as their interaction on %DLE and %R4h. In the quantitative modeling, the satisfactory adjustment of the linear models (along with interaction terms) with the experimental data for both %DLE and %R4h has confirmed the findings of the multivariate analysis. The optimized SS-loaded SA-PEC bubble beads based on 2D (contours), 3D, desirability, and overlay plots has exhibited %DLE of 87.35⯱â¯2.48% (nâ¯=â¯3 and errorâ¯=â¯2.94%) and %R4h of 85.79⯱â¯2.98% (nâ¯=â¯3 and errorâ¯=â¯0.25%). The in vitro drug release studies have shown almost complete (≥85%) SS release from all the batches within 4-6â¯h in simulated gastric fluid (SGF) pHâ¯1.2. The in vivo clinical findings by ultrasound studies have shown excellent floatation (>6â¯h) behavior of bubble beads in the upper gastrointestinal tract (GIT) and efficient stomach-specific gastroretention.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pectins
/
Drug Delivery Systems
/
Albuterol
/
Alginates
/
Adrenergic beta-2 Receptor Agonists
Type of study:
Diagnostic_studies
/
Prognostic_studies
Limits:
Humans
Language:
En
Journal:
Eur J Pharm Sci
Journal subject:
FARMACIA
/
FARMACOLOGIA
/
QUIMICA
Year:
2018
Document type:
Article
Affiliation country: