Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug-loaded chitosan microspheres

Giunchedi, Paolo; Juliano, Claudia Clelia Assunta; Gavini, Elisabetta; Cossu, Massimo; Sorrenti, Milena

doi:10.1016/s0939-6411(01)00237-5

Cited by 152 publications

(72 citation statements)

References 18 publications

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“…7,17 Various buccal adhesive dosage forms, such as discs, microspheres, and bilayered tablets, have been thoroughly prepared and reported by several research groups. [11][12][13][14][15][16][17] However, limited studies exist on novel devices that are superior to those of conventional buccal adhesive systems for the delivery of therapeutic agents through buccal mucosa.This study reports a novel system for buccal drug delivery. The principal aim was to prepare and evaluate a NBAS.…”

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confidence: 99%

Preparation and evaluation of a novel buccal adhesive system

Desai

Kumar

2004

AAPS PharmSciTech

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The aim of the present study was to prepare and evaluate a novel buccal adhesive system (NBAS) containing propranolol hydrochloride (PH). A special punch was fabricated and used while preparing an NBAS. Solubility of PH in phosphate buffer solution (pH 6.6), partition coefficient between phosphate buffer (pH 6.6) and 1-octanol, and permeability coefficient through the porcine buccal mucosa were performed and found to be 74.66 mg/mL, 5.17, and 5.6, respectively. Stability of NBAS was determined in natural human saliva, and it was found that both PH and device are stable in human saliva. NBAS was evaluated by weight uniformity, thickness, hardness, friability, swelling, mucoadhesive strength, in vitro drug release, and in vivo human acceptability studies. Swelling index was higher (4.4) for formulations containing hydroxyl propyl methyl cellulose (HPMC) K4M alone, and it decreases with its decreasing concentration in the NBAS. Mucoadhesive strength (MS) was measured by using a modified apparatus. All NBASs showed higher MS with porcine buccal mucosa when compared with that of rabbit buccal mucosa. NBASs containing carbopol (CP) 934P and HPMC K4M at the ratio of 1:1 showed higher MS (44.76 g) with porcine buccal mucosa when compared with 1:2 (39.76 g), 0:1 (23.29 g), and 1:0 (22.22 g) ratios, respectively. The mechanism of PH release was found to be by non-Fickian diffusion (value of "n" between 0.5 and 1.0) and followed first order kinetics. In vivo human acceptability study showed that the newly prepared NBAS was comfortable in the human buccal cavity. It can be concluded that NBAS is a superior, novel system that overcomes the drawback associated with the conventional buccal adhesive tablet.KEYWORDS: buccal delivery, carbopol 934P, HPMC K4M, propranolol hydrochloride, mucoadhesion. INTRODUCTIONIn recent years, delivery of therapeutic agents through various transmucosal routes has gained significant attention owing to their presystemic metabolism or instability in the acidic environment associated with oral administration. [1][2][3][4][5] The oral mucosa can be categorized into sublingual, gingival, and buccal mucosa through which oral transmucosal delivery can be achieved. Absorption of therapeutic agents from the oral cavity provides a direct entry of such agents into the systemic circulation, thereby avoiding the first-pass hepatic metabolism and gastrointestinal degradation. 6-8 However, the buccal route of drug delivery has received much more attention because of its unique advantages over other oral transmucosal routes. 7,[9][10] Delivery of various therapeutic agents via the buccal route using conventional matrix tablets, films, bilayered systems, and hydrogel systems has been studied and reported by several research groups. 11-16 A number of formulation and processing factors can influence properties and release properties of the buccal adhesive system. The conventional buccal adhesive tablets have some limitations: (1) conventional tablets may not have a uniform adhesive layer, leading to weak ad...

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Preparation and evaluation of a novel buccal adhesive system

Desai

Kumar

2004

AAPS PharmSciTech

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“…In addition to its favorable properties, such as nontoxicity, biocompatibility, and biodegradability, CH has an extended retention time on the oral mucosa [25]. Moreover; CH itself has an antimicrobial activity [26].…”

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Comparative Evaluation of Clinical Efficacy of Chlorhexidine, Phenolic and Chitosan Mouthrinses on Plaque and Gingivitis: Single-Centre, Double Blind, Randomized Controlled Clinical Study

HP¹

2017

Austin J Dent

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The present study was conducted to determine the effect of different mouthwash preparations used as supplement to regular oral hygiene measures on plaque and gingivitis.A total of 40 patients with chronic gingivitis demonstrating good oral hygiene were recruited for the study and divided into 4 groups. The subjects were briefed about the nature of the study and informed consents were taken. 4 different mouthwash preparations were given among the 4 groups. They are chlorhexidine digluconate, phenolic (Essential oil), chitosan anti-adhesive mouthwash and placebo (distilled water) for the control group. Clinical parameters including gingival index (Loe-Silness, 1963), plaque index (Turesky modification of Quigley-Hein, 1970) and stain index (Lobene, 1968) were recorded at baseline, 3 weeks and 6 weeks for all 4 groups.Results showed that there is highly statistically significant decrease in plaque and gingival index in chlorhexidine and Essential oil group, statistically significant decrease in chitosan and placebo group. Findings from this study indicate chlorhexidine to be the most effective anti-plaque and anti-gingivitis agent, followed by Essential oil mouthwash with the benefit of reduced staining, thus can be used on long term basis, and whereas chitosan is not significantly effective compared to placebo group.

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“…87 Tabletes baseados em microesferas de quitosana contendo diacetato de clorexidina mostraram uma liberação prolongada do fármaco na cavidade bucal. 88 Sistemas de liberação de fármacos a partir de quitosana, tais como microesferas, lipossomas e géis, têm demonstrado possuir boas características bioadesivas e intumescem facilmente quando em contato com a mucosa nasal. Vários sais de quitosana (lactato, aspartato, glutamato e cloridrato de quitosana) mostraram liberação sustentada nasal do fármaco cloridrato de vincomicina.…”

Section: Sistemas De Liberação De Fármacos a Partir De Matrizes De Quunclassified

Quitosana: biopolímero funcional com potencial industrial biomédico

Laranjeira¹,

Fávere²

2009

Quím. Nova

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Recebido em 27/1/09; aceito em 13/3/09; publicado na web em 2/4/09 CHITOSAN: FUNCTIONAL BYOPOLYMER WITH BIOMEDICAL INDUSTRIAL POTENTIAL. The importance of chitosan has grown significantly over the last two decades due to its renewable and biodegradable source, and also because of the recent increase in the knowledge of its functionality in the technological and biomedical applications. The present article reviews the biopolymer chitosan and its derivatives as versatile biomaterials for potential drug delivery systems, as well as tissue engineering applications, analgesia and treatment of arthritis.

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Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug-loaded chitosan microspheres

Cited by 152 publications

References 18 publications

Preparation and evaluation of a novel buccal adhesive system

Preparation and evaluation of a novel buccal adhesive system

Comparative Evaluation of Clinical Efficacy of Chlorhexidine, Phenolic and Chitosan Mouthrinses on Plaque and Gingivitis: Single-Centre, Double Blind, Randomized Controlled Clinical Study

Quitosana: biopolímero funcional com potencial industrial biomédico

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