Comparison of the effects of various transmucosal absorption promoters on buccal insulin delivery

Aungst, Bruce J.; Rogers, Nancy J.

doi:10.1016/0378-5173(89)90316-5

Cited by 100 publications

(21 citation statements)

References 23 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%

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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%

“…Substances that facilitate the permeation through buccal mucosa are referred as permeation enhancers (12). Different types of potential permeation enhancers have been studied for buccal route to increase the penetration of drugs (13,14).…”

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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“…However, most of the drugs administered in the form of buccal or sublingual tablets have exhibited low bioavailability due to the low mucosal membrane permeability. In order to overcome this problem, one approach consists of increasing the permeability of the buccal mucosa using penetration enhancers, which are able to decrease the barrier capacity of the tissue (3)(4)(5)(6). The permeation enhancement approach was considered in order to further improve buccal mucosal membrane permeability of various drug delivery systems (7)(8)(9).…”

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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“…They have often been used to enhance the absorption of insulin across the mucous membranes from various sites. 16,32,33) As bile salts can serve as enhancers, sodium deoxycholate not entrapped into the vesicles may enhance the absorption of insulin across the buccal membrane. On the other hand, bile salts not only act as enhancers, but also they play an important role in preparing the deformable vesicles with special characteristics.…”

Section: Discussionmentioning

confidence: 99%

Phospholipid Deformable Vesicles for Buccal Delivery of Insulin.

Yang

Wang

Yan

et al. 2002

CHEMICAL & PHARMACEUTICAL BULLETIN

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To investigate the possibility of the enhancing effect of deformable vesicles on buccal delivery of insulin, two kinds of vesicles with and without the presence of sodium deoxycholate (deformable vesicles and conventional vesicles) were prepared by reverse phase evaporation methods. The liposomal entrapment efficiency was determined by column chromatography. The particle size and morphology of the vesicles were also evaluated. The hypoglycemic effects, insulin concentrations, and residual amounts of insulin deposited in the buccal membrane after buccal administration of insulin vesicles to rabbits were investigated. Compared with subcutaneous administration of insulin solution, the relative pharmacological bioavailability and the relative bioavailability of buccal administration of insulin vesicles were determined. The results showed that the entrapment efficiencies of the deformable and conventional vesicles were 18.87؎1.78% (n‫)3؍‬ and 22.07؎2.16% (n‫,)3؍‬ respectively. The particle sizes of the deformable and conventional vesicles were 42.5؎20.5 nm and 59.7؎33.8 nm, respectively. There were no significant differences in appearance between the two types of vesicle. Compared with subcutaneous administration of insulin solution, the relative pharmacological bioavailability and the relative bioavailability in the insulin-deformable vesicles group were 15.59% and 19.78%, respectively, which were higher than in the conventional insulin vesicles (pϽ0.05), blank deformable vesicles and insulin mixture groups (pϽ0.05). Deformable vesicles have an enhancing effect on buccal delivery of insulin and may be a better carrier than conventional vesicles for buccal delivery of protein drugs.

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Comparison of the effects of various transmucosal absorption promoters on buccal insulin delivery

Cited by 100 publications

References 23 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

Phospholipid Deformable Vesicles for Buccal Delivery of Insulin.

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