In the present work we investigated the feasibility of chitosan treated Ca-alginate microparticles for delivery of naproxen in lower parts of GIT and evaluated influence of formulation factors on their physicochemical characteristics and drug release profiles. Investigated factors were drug/polymer ratio, chitosan molecular weight, chitosan concentration in hardening medium, and hardening time. Sixteen microparticle formulations were prepared utilizing 24 full factorial design (each factor was varied at two levels). Microparticles size varied between 262.3 +/- 14.9 and 358.4 +/- 21.7 mu m with slightly deformed spherical shape. Low naproxen solubility and rapid reaction of ionotropic gelation resulted in high encapsulation efficiency (> 75.19%). Under conditions mimicking those in the stomach, after two hours, less than 6.18% of naproxen was released. Significant influence of all investigated factors on drug release rate was observed in simulated small intestinal fluid. Furthermore, ex...perimental design analysis revealed that chitosan molecular weight and its concentration had the most pronounced effect on naproxen release. Release data kinetics indicated predominant influence of a pH-dependent relaxation mechanism on drug release from microparticles.
TY - JOUR
AU - Čalija, Bojan
AU - Cekić, Nebojša
AU - Savić, Snežana
AU - Krajišnik, Danina
AU - Daniels, Rolf
AU - Milić, Jela
PY - 2011
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1558
AB - In the present work we investigated the feasibility of chitosan treated Ca-alginate microparticles for delivery of naproxen in lower parts of GIT and evaluated influence of formulation factors on their physicochemical characteristics and drug release profiles. Investigated factors were drug/polymer ratio, chitosan molecular weight, chitosan concentration in hardening medium, and hardening time. Sixteen microparticle formulations were prepared utilizing 24 full factorial design (each factor was varied at two levels). Microparticles size varied between 262.3 +/- 14.9 and 358.4 +/- 21.7 mu m with slightly deformed spherical shape. Low naproxen solubility and rapid reaction of ionotropic gelation resulted in high encapsulation efficiency (> 75.19%). Under conditions mimicking those in the stomach, after two hours, less than 6.18% of naproxen was released. Significant influence of all investigated factors on drug release rate was observed in simulated small intestinal fluid. Furthermore, experimental design analysis revealed that chitosan molecular weight and its concentration had the most pronounced effect on naproxen release. Release data kinetics indicated predominant influence of a pH-dependent relaxation mechanism on drug release from microparticles.
PB - Pharmaceutical Soc Korea, Seoul
T2 - Archives of Pharmacal Research
T1 - An investigation of formulation factors affecting feasibility of alginate-chitosan microparticles for oral delivery of naproxen
VL - 34
IS - 6
SP - 919
EP - 929
DO - 10.1007/s12272-011-0609-y
ER -
@article{
author = "Čalija, Bojan and Cekić, Nebojša and Savić, Snežana and Krajišnik, Danina and Daniels, Rolf and Milić, Jela",
year = "2011",
abstract = "In the present work we investigated the feasibility of chitosan treated Ca-alginate microparticles for delivery of naproxen in lower parts of GIT and evaluated influence of formulation factors on their physicochemical characteristics and drug release profiles. Investigated factors were drug/polymer ratio, chitosan molecular weight, chitosan concentration in hardening medium, and hardening time. Sixteen microparticle formulations were prepared utilizing 24 full factorial design (each factor was varied at two levels). Microparticles size varied between 262.3 +/- 14.9 and 358.4 +/- 21.7 mu m with slightly deformed spherical shape. Low naproxen solubility and rapid reaction of ionotropic gelation resulted in high encapsulation efficiency (> 75.19%). Under conditions mimicking those in the stomach, after two hours, less than 6.18% of naproxen was released. Significant influence of all investigated factors on drug release rate was observed in simulated small intestinal fluid. Furthermore, experimental design analysis revealed that chitosan molecular weight and its concentration had the most pronounced effect on naproxen release. Release data kinetics indicated predominant influence of a pH-dependent relaxation mechanism on drug release from microparticles.",
publisher = "Pharmaceutical Soc Korea, Seoul",
journal = "Archives of Pharmacal Research",
title = "An investigation of formulation factors affecting feasibility of alginate-chitosan microparticles for oral delivery of naproxen",
volume = "34",
number = "6",
pages = "919-929",
doi = "10.1007/s12272-011-0609-y"
}
Čalija, B., Cekić, N., Savić, S., Krajišnik, D., Daniels, R.,& Milić, J.. (2011). An investigation of formulation factors affecting feasibility of alginate-chitosan microparticles for oral delivery of naproxen. in Archives of Pharmacal Research
Pharmaceutical Soc Korea, Seoul., 34(6), 919-929.
https://doi.org/10.1007/s12272-011-0609-y
Čalija B, Cekić N, Savić S, Krajišnik D, Daniels R, Milić J. An investigation of formulation factors affecting feasibility of alginate-chitosan microparticles for oral delivery of naproxen. in Archives of Pharmacal Research. 2011;34(6):919-929.
doi:10.1007/s12272-011-0609-y .
Čalija, Bojan, Cekić, Nebojša, Savić, Snežana, Krajišnik, Danina, Daniels, Rolf, Milić, Jela, "An investigation of formulation factors affecting feasibility of alginate-chitosan microparticles for oral delivery of naproxen" in Archives of Pharmacal Research, 34, no. 6 (2011):919-929,
https://doi.org/10.1007/s12272-011-0609-y . .
