35 Citations (Scopus)

Abstract

In this study, the release characteristics of lidocaine conveyed in base (LB) and salt (LS) forms from an anionic hydrogel composed of carbopol and a cationic hydrogel composed of chitosans were examined for optimizing hydrogel formulation as a sponge filler to stop the bleeding and as a carrier for delivering lidocaine to relief pain after a tooth extraction. A Franz cell was used to simulate the in vivo environment and evaluate the drug release kinetics. It was confirmed that the release profiles of LB and LS from both the carbopol and chitosan hydrogels were best described by the Higuchi model, and values of the release rate constant (K) calculated from the slope of the linear portion of the plot were compared. Results demonstrated that the K value increased with increasing LB concentration at the same three carbopol levels of the hydrogels, whereas it increased with a decreasing level of carbopol for the same concentration of LB in the hydrogels. A minimum in the value of K was observed near neutral pH, which was attributed to two influencing factors of the viscosity and the complexing effect of carbopol gel. However, K values at the same concentration of lidocaine were larger for those formulations using the salt form compared to those using the base form. Results further revealed that the K value increased with an increasing amount of LB added to chitosan hydrogels with the same 0.5% concentration of C1000 (Chitosan, viscosity 1000 cps). K values increased with a decreasing MW of chitosan at the same level in the same concentration of an acetic acid solution with the same amount of LB added. K values for the release from chitosan hydrogels prepared at a lower level were lower than those of hydrogels prepared at a higher level. However, similarities in the release profiles between LB and LS were observed. In conclusion, the viscosity of the gel matrix and the ionic complexing effect between the anionic acid groups of hydrogels and basic groups with lidocaine were two main factors influencing regulation of the diffusion coefficient for controlling drug release.

Original languageEnglish
Pages (from-to)333-339
Number of pages7
JournalJournal of Controlled Release
Volume118
Issue number3
DOIs
Publication statusPublished - Apr 23 2007

Fingerprint

Hydrogels
Lidocaine
Chitosan
Hydrogel
Salts
Viscosity
Gels
Tooth Extraction
Porifera
Acetic Acid
Pharmacokinetics
carboxypolymethylene
Hemorrhage
Pain
Acids

Keywords

  • Carbopol
  • Chitosan
  • Hydrogel
  • Lidocaine
  • Release characteristics

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Release characteristics of lidocaine from local implant of polyanionic and polycationic hydrogels. / Liu, Der Zen; Sheu, Ming Thau; Chen, Chien Ho; Yang, You Ren; Ho, Hsiu O.

In: Journal of Controlled Release, Vol. 118, No. 3, 23.04.2007, p. 333-339.

Research output: Contribution to journalArticle

@article{454a49f9e2ce49c2b9485cbe770563f4,
title = "Release characteristics of lidocaine from local implant of polyanionic and polycationic hydrogels",
abstract = "In this study, the release characteristics of lidocaine conveyed in base (LB) and salt (LS) forms from an anionic hydrogel composed of carbopol and a cationic hydrogel composed of chitosans were examined for optimizing hydrogel formulation as a sponge filler to stop the bleeding and as a carrier for delivering lidocaine to relief pain after a tooth extraction. A Franz cell was used to simulate the in vivo environment and evaluate the drug release kinetics. It was confirmed that the release profiles of LB and LS from both the carbopol and chitosan hydrogels were best described by the Higuchi model, and values of the release rate constant (K) calculated from the slope of the linear portion of the plot were compared. Results demonstrated that the K value increased with increasing LB concentration at the same three carbopol levels of the hydrogels, whereas it increased with a decreasing level of carbopol for the same concentration of LB in the hydrogels. A minimum in the value of K was observed near neutral pH, which was attributed to two influencing factors of the viscosity and the complexing effect of carbopol gel. However, K values at the same concentration of lidocaine were larger for those formulations using the salt form compared to those using the base form. Results further revealed that the K value increased with an increasing amount of LB added to chitosan hydrogels with the same 0.5{\%} concentration of C1000 (Chitosan, viscosity 1000 cps). K values increased with a decreasing MW of chitosan at the same level in the same concentration of an acetic acid solution with the same amount of LB added. K values for the release from chitosan hydrogels prepared at a lower level were lower than those of hydrogels prepared at a higher level. However, similarities in the release profiles between LB and LS were observed. In conclusion, the viscosity of the gel matrix and the ionic complexing effect between the anionic acid groups of hydrogels and basic groups with lidocaine were two main factors influencing regulation of the diffusion coefficient for controlling drug release.",
keywords = "Carbopol, Chitosan, Hydrogel, Lidocaine, Release characteristics",
author = "Liu, {Der Zen} and Sheu, {Ming Thau} and Chen, {Chien Ho} and Yang, {You Ren} and Ho, {Hsiu O.}",
year = "2007",
month = "4",
day = "23",
doi = "10.1016/j.jconrel.2007.01.001",
language = "English",
volume = "118",
pages = "333--339",
journal = "Journal of Controlled Release",
issn = "0168-3659",
publisher = "Elsevier",
number = "3",

}

TY - JOUR

T1 - Release characteristics of lidocaine from local implant of polyanionic and polycationic hydrogels

AU - Liu, Der Zen

AU - Sheu, Ming Thau

AU - Chen, Chien Ho

AU - Yang, You Ren

AU - Ho, Hsiu O.

PY - 2007/4/23

Y1 - 2007/4/23

N2 - In this study, the release characteristics of lidocaine conveyed in base (LB) and salt (LS) forms from an anionic hydrogel composed of carbopol and a cationic hydrogel composed of chitosans were examined for optimizing hydrogel formulation as a sponge filler to stop the bleeding and as a carrier for delivering lidocaine to relief pain after a tooth extraction. A Franz cell was used to simulate the in vivo environment and evaluate the drug release kinetics. It was confirmed that the release profiles of LB and LS from both the carbopol and chitosan hydrogels were best described by the Higuchi model, and values of the release rate constant (K) calculated from the slope of the linear portion of the plot were compared. Results demonstrated that the K value increased with increasing LB concentration at the same three carbopol levels of the hydrogels, whereas it increased with a decreasing level of carbopol for the same concentration of LB in the hydrogels. A minimum in the value of K was observed near neutral pH, which was attributed to two influencing factors of the viscosity and the complexing effect of carbopol gel. However, K values at the same concentration of lidocaine were larger for those formulations using the salt form compared to those using the base form. Results further revealed that the K value increased with an increasing amount of LB added to chitosan hydrogels with the same 0.5% concentration of C1000 (Chitosan, viscosity 1000 cps). K values increased with a decreasing MW of chitosan at the same level in the same concentration of an acetic acid solution with the same amount of LB added. K values for the release from chitosan hydrogels prepared at a lower level were lower than those of hydrogels prepared at a higher level. However, similarities in the release profiles between LB and LS were observed. In conclusion, the viscosity of the gel matrix and the ionic complexing effect between the anionic acid groups of hydrogels and basic groups with lidocaine were two main factors influencing regulation of the diffusion coefficient for controlling drug release.

AB - In this study, the release characteristics of lidocaine conveyed in base (LB) and salt (LS) forms from an anionic hydrogel composed of carbopol and a cationic hydrogel composed of chitosans were examined for optimizing hydrogel formulation as a sponge filler to stop the bleeding and as a carrier for delivering lidocaine to relief pain after a tooth extraction. A Franz cell was used to simulate the in vivo environment and evaluate the drug release kinetics. It was confirmed that the release profiles of LB and LS from both the carbopol and chitosan hydrogels were best described by the Higuchi model, and values of the release rate constant (K) calculated from the slope of the linear portion of the plot were compared. Results demonstrated that the K value increased with increasing LB concentration at the same three carbopol levels of the hydrogels, whereas it increased with a decreasing level of carbopol for the same concentration of LB in the hydrogels. A minimum in the value of K was observed near neutral pH, which was attributed to two influencing factors of the viscosity and the complexing effect of carbopol gel. However, K values at the same concentration of lidocaine were larger for those formulations using the salt form compared to those using the base form. Results further revealed that the K value increased with an increasing amount of LB added to chitosan hydrogels with the same 0.5% concentration of C1000 (Chitosan, viscosity 1000 cps). K values increased with a decreasing MW of chitosan at the same level in the same concentration of an acetic acid solution with the same amount of LB added. K values for the release from chitosan hydrogels prepared at a lower level were lower than those of hydrogels prepared at a higher level. However, similarities in the release profiles between LB and LS were observed. In conclusion, the viscosity of the gel matrix and the ionic complexing effect between the anionic acid groups of hydrogels and basic groups with lidocaine were two main factors influencing regulation of the diffusion coefficient for controlling drug release.

KW - Carbopol

KW - Chitosan

KW - Hydrogel

KW - Lidocaine

KW - Release characteristics

UR - http://www.scopus.com/inward/record.url?scp=33947324513&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33947324513&partnerID=8YFLogxK

U2 - 10.1016/j.jconrel.2007.01.001

DO - 10.1016/j.jconrel.2007.01.001

M3 - Article

C2 - 17292505

AN - SCOPUS:33947324513

VL - 118

SP - 333

EP - 339

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

IS - 3

ER -