Design and characteristics of gellan gum beads for modified release of meloxicam

被引:11
|
作者
Osmalek, Tomasz [1 ]
Milanowski, Bartlomiej [1 ]
Froelich, Anna [1 ]
Szybowicz, Miroslaw [2 ]
Bialowas, Wojciech [1 ]
Kapela, Marcin [1 ]
Gadzinski, Piotr [1 ]
Ancukiewicz, Katarzyna [1 ]
机构
[1] Poznan Univ Med Sci, Dept Pharmaceut Technol, Grunwaldzka 6, PL-60780 Poznan, Poland
[2] Poznan Univ Tech, Fac Tech Phys, Poznan, Poland
关键词
Meloxicam; gellan gum; ionotropic gelation; drug release; Design of Experiments; IN-VITRO RELEASE; FERMENTATIVE PRODUCTION; BETA-CYCLODEXTRIN; FLOATING BEADS; ALGINATE BEADS; DRUG-DELIVERY; FORMULATIONS; ACID; BIOSYNTHESIS; CANCER;
D O I
10.1080/03639045.2017.1318896
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The aim of the presented work was to design, formulate and evaluate the properties of low-acyl gellan macro beads with the potential application as carriers for oral delivery of meloxicam (MLX) in the prophylaxis of colorectal cancer. The beads were obtained by means of ionotropic gelation technique. Calcium chloride (1.0%, 9.0 x 10(-2) M) was used as the cross-linking agent. Nine different polymer, drug and surfactant (Tween (R) 80) mixtures were used for production of the beads. The quantitative compositions of the mixtures were generated with the application of the Design of Experiments (DoE) modulus from the STATISTICA Software. The prepared formulations revealed 7.2-27.0% of drug loading and 29.2-50.7% drug encapsulation efficiency. It turned out that 0.5% amount of gellan gum in the mixtures was not sufficient to obtain spherical beads. The morphology and surface of the dried beads were analyzed by SEM. Raman spectra confirmed that MLX did not undergo structural changes during production of the beads. The swelling behavior and degradation of the beads were evaluated in three simulated gastrointestinal fluids at different pH (1.2; 4.5; 6.8). The MLX in vitro release studies were conducted on USP apparatus IV, working in the open loop mode. The obtained results showed that MLX release from the dried beads was pH-dependent. The formulations obtained from mixtures containing 1.0 and 1.5% of gellan may be considered as oral dosage forms for MLX, intended to omit the stomach and release the drug in the distal parts of the gastrointestinal tract.
引用
收藏
页码:1314 / 1329
页数:16
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