Eudragit®-S100 Coated PLGA Nanoparticles for Colon Targeting of Etoricoxib: Optimization and Pharmacokinetic Assessments in Healthy Human Volunteers

被引:21
|
作者
El-Maghawry, Enas [1 ]
Tadros, Mina, I [2 ]
Elkheshen, Seham A. [2 ]
Abd-Elbary, Ahmed [2 ]
机构
[1] Future Univ Egypt, Fac Pharmaceut Sci & Pharmaceut Ind, Dept Pharmaceut & Pharmaceut Technol, Cairo, Egypt
[2] Cairo Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11562, Egypt
来源
关键词
colon targeting; etoricoxib; nano spray drying; PLGA; Eudragit-S100; DRUG-DELIVERY SYSTEM; IN-VITRO EVALUATION; FORMULATION VARIABLES; RELEASE; MICROSPHERES; DESIGN; PROTEIN; DEGRADATION; GLYCOLIDE; INHIBITOR;
D O I
10.2147/IJN.S244124
中图分类号
TB3 [工程材料学];
学科分类号
0805 ; 080502 ;
摘要
Aim: Etoricoxib is a selective inhibitor of COX-2 enzyme. It is proposed as a potent anti-inflammatory drug intended for the control of irritable bowel syndrome. The current work aimed at developing etoricoxib-loaded nanoparticles for colon- targeting. Materials and Methods: PLGA nanoparticles were developed via nano-spray drying technique. The D-optimal design was adopted for the investigation of the influence of i) DL-lactide-coglycolide (PLGA) concentration, ii) polyvinylpyrrolidone K30 (PVP K30) concentration and iii) lactide:glycolide ratio in the copolymer chain on the yield%, the encapsulation efficiency (EE %), particle size (PS) and percentage of drug release after 2h (P-2h), 4h (P-4h) and 12h (P-12h). To promote colon targeting of the systems, the best achieved system (M14) was either directly coated with poly(methacrylic acid-co-methyl methacrylate) [Eudragit (R)-S100] or loaded into hard gelatin capsules and the capsules were coated with poly(methacrylic acid-co-methyl methacrylate) (E-M14C). The pharmacokinetic parameters of etoricoxib following oral administration of E-M14C in healthy volunteers were assessed relative to commercial etoricoxib tablets. Results: M14 system was prepared using PLGA (0.5% w/v) at a lactide:glycolide ratio of 100:0, in the presence of PVP K30 (2% w/v). M14 system was nano-spherical particles of 488 nm size possessing promising yield% (63.5%) and EE% (91.2%). The percentage drug released after 2, 4 and 12 hours were 43.41%, 47.34 and 64.96%, respectively. Following M14-loading into hard gelatin capsules and coating with poly(methacrylic acid-co-methyl methacrylate) [Eudragit-S100], the respective P-2h, P-4h and P-12h were 10.1%, 28.60% and 65.45%. Significant (p < 0.05) differences between the pharmacokinetic parameter of E-M14C in comparison with the commercial product were revealed with a delay in T-max (from 2.5h to 6h), a prolongation in MRT0-infinity (from 24.4h to 34.7h) and an increase in the relative oral bioavailability (4.23 folds). Conclusion: E-M14C is a potential system for possible colon targeting of etoricoxib.
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收藏
页码:3965 / 3980
页数:16
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