An in vivo dog model for studying recovery kinetics of the buccal mucosa permeation barrier after exposure to permeation enhancers: apparent evidence of effective enhancement without tissue damage

Zhang, Jie; Niu, Suyi; Ebert, C. D.; Stanley, Theodore H.

doi:10.1016/0378-5173(94)90071-x

Cited by 41 publications

(14 citation statements)

References 11 publications

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“…The delivery of hydrophilic macromolecular drugs via buccal membrane was made possible by incorporation of absorption or permeation enhancers, which could reduce barrier properties of the buccal epithelium (13)(14)(15)(16)(17)(18)(19)(20).…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Bioadhesive Buccal Drug Delivery of Tizanidine Hydrochloride Tablets

Shanker

Kumar²,

Gonugunta

et al. 2009

AAPS PharmSciTech

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Abstract. The study aim was concerned with formulation and evaluation of bioadhesive buccal drug delivery of tizanidine hydrochloride tablets, which is extensively metabolized by liver. The tablets were prepared by direct compression using bioadhesive polymers such as hydroxylpropyl methylcellulose K4M, sodium carboxymethyl cellulose alone, and a combination of these two polymers. In order to improve the permeation of drug, different permeation enhancers like beta-cyclodextrin (β-CD), hydroxylpropyl beta-cyclodextrin (HP-β-CD), and sodium deoxycholate (SDC) were added to the formulations. The β-CD and HP-β-CD were taken in 1:1 molar ratio to drug in formulations. Bioadhesion strength, ex vivo residence time, swelling, and in vitro dissolution studies and ex vivo permeation studies were performed. In vitro release of optimized bioadhesive buccal tablet was found to be non-Fickian. SDC was taken in 1%, 2%, and 3% w/w of the total tablet weight. Stability studies in natural saliva indicated that optimized formulation has good stability in human saliva. In vivo mucoadhesive behavior of optimized formulation was performed in five healthy male human volunteers and subjective parameters were evaluated.KEY WORDS: bioadhesive buccal tablets; in vitro evaluation; in vivo mucoadhesive behavior; permeation enhancers; stability studies in natural saliva; tizanidine hydrochloride.

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Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Bioadhesive Buccal Drug Delivery of Tizanidine Hydrochloride Tablets

Shanker

Kumar²,

Gonugunta

et al. 2009

AAPS PharmSciTech

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“…The permeation enhancement approach was considered in order to further improve buccal mucosal membrane permeability of various drug delivery systems (7)(8)(9). However, it is unclear whether they act by transiently altering the mucosa or by damaging it (10).…”

Section: Introductionmentioning

confidence: 99%

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

Dhiman

Dhiman²,

Sawant

2009

AAPS PharmSciTech

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Abstract. The purpose of this study was to determine the effect of permeation enhancers on the transbuccal delivery of 5-fluorouracil (FU). The effect of permeation enhancers on in vitro buccal permeability was assessed using sodium deoxycholate (SDC), sodium dodecyl sulphate (SDS), sodium tauroglycocholate (STGC), and oleic acid and their concentrations for absorption enhancement were optimized. STGC appeared to be most effective for enhancing the buccal permeation of FU than the other enhancers. These enhancements by STGC were statistically significant (p<0.05) compared to control. The order of permeation enhancement was STGC > SDS > SDC > oleic acid. Histological investigations were performed on buccal mucosa and indicated no major morphological changes. The enhancing effect of STGC on the buccal absorption of FU was evaluated from the mucoadhesive gels in rabbits. The absolute bioavailability of FU from mucoadhesive gels containing STGC increased 1.6-fold as compared to the gels containing no permeation enhancer. The mean residence time and mean absorption time considerably increased following administration of gel containing penetration enhancer compared with the gel without penetration enhancer.

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“…At regular 1-hour time intervals until 3 hours, patches are removed from the gel plates and excess surface water is removed carefully using the filter paper. 46 The swollen patches are then reweighed (W2) and the swelling index (SI) is calculated using the following formula.…”

Section: Swelling Studymentioning

confidence: 99%

“…Hot-melt extrusion [35][36][37] In hot-melt extrusion, A blend of pharmaceutical ingredients is molten.…”

Section: 92mentioning

confidence: 99%

A Review on Promising Novel Drug delivery System - Bioadhesive Drug Delivery System

Dave

Mishra

2017

Curr. Res. Pharm. Sci.

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Bioadhesive drug delivery system has gained sufficient attention of researchers not only due to their enormous advantages but also feasibility of formulation and patient compliance. In this review an effort was made to describe aspects of bioadhesive films, their preparation methods, polymer used in the formulation of this type of drug delivery system, different mechanism of how plasticizer work in drug delivery films and different evaluation parameters of this type of formulation so that this can be further studied and formulated with wide spectrum drug by checking suitability of the formulation with the active pharmaceutical ingredient.

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An in vivo dog model for studying recovery kinetics of the buccal mucosa permeation barrier after exposure to permeation enhancers: apparent evidence of effective enhancement without tissue damage

Cited by 41 publications

References 11 publications

Formulation and Evaluation of Bioadhesive Buccal Drug Delivery of Tizanidine Hydrochloride Tablets

Formulation and Evaluation of Bioadhesive Buccal Drug Delivery of Tizanidine Hydrochloride Tablets

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

A Review on Promising Novel Drug delivery System - Bioadhesive Drug Delivery System

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