Buccal Patches Research Articles

Atenolol-releasing buccal patches made of Dillenia indica L. fruit gum: preparation and ex vivo evaluations

The objective of present research deals with the utility of extracted dillenia fruit gum (DG) as pharmaceutical excipient in the formulation of buccal patches containing atenolol (for the use in the treatment of hypertension). The atenolol-releasing buccal patches having a mucoadhesive polymeric layer of extracted DG-hydroxypropyl methylcellulose (HPMC K4M) and a drug-free backing layer of ethyl cellulose (1%) were prepared through the solvent-casting process. Various physicochemical parameters such as drug content, average weight, thickness, folding endurance and moisture content of all these buccal patches were found satisfactory. Ex vivo buccoadhesion was also found satisfactory. Ex vivo drug permeation across the excised porcine buccal mucosal membrane demonstrated the atenolol permeation over 12 h, which obeyed the first-order model (R2 = 0.9858–0.9967) with non-Fickian (anomalous) diffusion mechanism (n = 0.72–0.75). These buccal patches were also characterized by SEM and FTIR spectroscopy. These atenolol-releasing buccal patches can be used in the treatment of hypertension and angina pectoris bypassing the extensive hepatic first-pass metabolism.

OVERVIEW OF MUCOADHESIVE BIOPOLYMERS FOR BUCCAL DRUG DELIVERY SYSTEMS

Mucoadhesive dosage forms may be intended for facilitation of prolonged retention time at the application site hence providing drug release in a controlled rate for enhanced improvement of therapeutic activity and its outcome. The buccal mucosa has been investigated for systemic drug delivery and local drug treatment or therapy that is subjected to first pass metabolism. The applicability of bio-adhesion approach in buccal drug delivery proved great therapeutic potential to overcome the limitation of conventional buccal drug delivery. The delivery via buccal route using mucoadhesive biopolymers such as various natural gums e.g. carrageenans, gum karaya, gum arabic, locust bean gum, khaya gum, gum ghatti, albizia gum, guar gum, starch, cellulose, larch gum and pectin etc. and various thiolated and carboxymethylated polymers has been the subject of interest since the early 20th century. The present article is focused mainly on the oral mucosa, mechanism of drug permeation, and characteristics of the desired polymers, the manuscript then proceeds to cover the theories behind the adhesion of bioadhesive polymers to the mucosal epithelium followed by the factors affecting mucoadhesion. Further the author has also discussed on the new generation of mucoadhesive polymers and their properties, recent mucoadhesive formulations for enhanced buccal drug delivery, various marketed products and patent literature. Various online search engines and scientific journals were employed for the collection of literature and scientific data and information related to the topic using keywords like mucoadhesive polymers, buccal drug delivery, buccal patches, tablets, films, gels, powder from the year 2002 and above.

DEVELOPMENT, EVALUATION, AND CHARACTERIZATION OF LOSARTAN POTASSIUM BUCCAL PATCHES USING JACKFRUIT POLYMER

Objective: The objective was to develop buccal patches of an antihypertensive drug and losartan potassium using jackfruit polymer for sustained buccal delivery.
 Methods: The patches were prepared by the solvent casting method. Five formulations were developed with varying concentrations of jackfruit polymer. USP type II apparatus was used to perform in-vitro release study under perfect sink condition. Buccal formulations were developed to a satisfactory level in terms of drug release, bioadhesive strength, content uniformity, moisture content, surface pH, thickness, and stability study.
 Results: From the results obtained F5 was found as best formulation, having appropriate folding endurance greater than 300, moisture content of 1.14±0.03 percentage (%), moisture uptake of 6.21±0.12%, swelling index (62.78%), bioadhesion strength (37.62±0.25 g), and bioadhesion time of 9 h 5 min. Fourier-transform infrared spectroscopy studies have shown no interactions between drug and polymer. All the formulations followed zero-order kinetics.
 Conclusion: It can be concluded that mucoadhesive buccal patches of losartan potassium using jackfruit polymer are an auspicious dosage form to prolong the release of drug and enhance its poor oral bioavailability.

Optimization of Unidirectional Mucoadhesive Buccal Patches Based on Chitosan and Pluronic® F-127 for Metoprolol Controlled Release: In Vitro and Ex Vivo Evaluations

The aim of this work was to optimize unidirectional buccal patches loaded with metoprolol (MT-MBPs) to provide adequate mucoadhesive and water uptake properties as well as controlled drug release for the effective treatment of different cardiovascular diseases. The patches were prepared layer-by-layer using the solvent casting method. A central composite design was employed to statistically optimize the formulation variables. Chitosan and Pluronic® F-127 (poloxamer 407) concentrations were chosen as the independent variables, while ex vivo mucoadhesive force, ex vivo residence time, in vitro water uptake (%), and in vitro drug release (%) were to be considered the dependent variables. The optimized formulation was also characterized and evaluated in terms of morphology, thermal behavior, tensile strength, elongation at break, and ex vivo drug permeation. The optimized MT-MBPs were successful in terms of mucoadhesive force (3.58 ± 0.62 N), residence time (342.67 ± 17.21 min), and water uptake at 1 h (24.53 ± 3.62%). A controlled drug release was obtained for 8 h. Thermal and morphologic analyses demonstrated that metoprolol was homogeneously distributed throughout the microporous chitosan-based polymer matrix. Furthermore, the MT-MBPs exhibited a tensile strength of 3.76 ± 0.55 N/mm2 and an elongation at break of 36.52 ± 13.88%. The results of ex vivo permeation through pig buccal mucosa indicated that therapeutic metoprolol concentrations can be reached by using a patch of 5.62 cm2. Optimal composition of the MT-MBPs included 2.9% (w/v) and 2.6% (w/v) of chitosan and Pluronic® F-127, respectively, which constitutes the most suitable makeup for metoprolol buccal delivery.

FORMULATION AND EVALUATION OF LORAZEPAM ENCAPSULATED COLLAGEN/PECTIN BUCCAL PATCH

Objective: To formulate and characterize Lorazepam loaded buccal patches using mucoadhesive, biodegradable, natural polymers-pectin (hydrophilic) and collagen (lipophilic) for treating epileptic seizures.
 Methods: Lorazepam loaded buccal patches were prepared by solvent casting method and were subjected to various Physico-chemical evaluation parameters to find the optimized buccal patch. The in vitro drug release study and ex vivo permeation study was carried out. The stability study and histopathological study of optimized Lorazepam loaded buccal patch was also carried out.
 Results: From in vitro drug release study, it was found that Lorazepam loaded buccal patch (B4) exhibited maximum drug release of 96.16 %±0.07 than other formulations at the end of 4 h, indicating an initial burst release followed by sustained release with release kinetics as Higuchi diffusion model. Based on the in vitro drug release, % drug content, % swelling index, folding endurance, B4 formulation was considered as optimised formulation and was further characterized. Ex vivo permeation study revealed that the cumulative amount of drug permeated from optimised Lorazepam loaded buccal patch (B4) was higher (3831.4±0.21µg/cm2) than marketed Midazolam buccal solution (1724±0.12 µg/cm2) and control drug solution (895.42±0.07 µg/cm2) with an enhancement ratio of 4.8. B4 formulation also showed a higher flux value (12.52±0.02µg/cm2/hr) compared to marketed formulation (5.732±0.01 µg/cm2) and control drug solution (2.563±0.03 µg/cm2) of P<0.05. The histopathological study using bovine buccal mucosa revealed that the B4 formulation is safe for buccal application. The stability study confirmed that B4 formulation is stable in both room and refrigeration conditions. Hence the formulated Lorazepam loaded buccal patch seems to be a promising carrier for the enhanced buccal delivery of Lorazepam in treating epileptic seizures.
 Conclusion: The formulated Lorazepam loaded collagen/pectin buccal patch was found to be an efficient and stable route for the buccal delivery of Lorazepam in treating acute epileptic seizures which could be further explored scientifically.

TRANSBUCCAL DELIVERY OF SPRAY DRIED LOVASTATIN FROM MUCOADHESIVE BUCCAL PATCHES AND IN VITRO CHARACTERIZATION

Objective: The aim of the present work was to develop and characterize mucoadhesive film of spray dried Lovastatin (LVS) for buccal delivery to enhance bioavailability.
 Methods: Mucoadhesive films were prepared by solvent casting technique by using different polymers HPMCK4M, HPMC E5LV and chitosan. The successful patches were evaluated for film thickness, weight, content uniformity, surface pH, swelling index, folding endurance, ex-vivo residence time, ex-vivo bioadhesion test, in vitro drug release, ex-vivo drug permeation and stability study.
 Results: The thickness of all prepared patches ranged from 0.21±0.07 to 1.5±0.39 mm, the weight of the film 89.10±0.6 to 128.57±0.3 mg, drug content 85.47±0.87 to 97.33±0.31%, surface pH 5.6±0.67 to 7.6±0.98, swelling index 23.0±4.1 to 76.5±3.6%, folding endurance 165±1.9 to 350±2.5 respectively. Ex-vivo residence time ranged from 2.2±0.08to 8.2±0.17 h and ex-vivo bioadhesive strength 30±0.64 to 66±0.43 g. The formulations with HPMC E5 shown short period of residence time and shows weak force of adhesion., which might be because of low viscosity of the polymer which resulted into weak adhesion. The percentage drug release and ex-vivo drug permeation was in the following descending order HPMC K4M>HPMC E5LV>chitosan. These results confirm the extension of drug release in case of ionic polymer chitosan. The kinetics data shows that drug release and permeation follows nonfiction diffusion. Accelerated stability data revealed that there is no significant change in drug content, in vitro drug release and ex-vivo permeation.
 Conclusion: It can be concluded that mucoadhesive buccal patch is a promising dosage form to enhance the drug bioavailability by preventing first-pass metabolism thus providing better therapeutic efficacy.

Mucoadhesive Buccal Patches: The Newest Way of Oral Drug Delivery

Buccal route has been an eye catching route for delivery of drugs. Presence of saliva, mucus makes buccal cavity more efficient for large number of drugs to administer through it for proper dissolution and bioavailability without facing enzymatic degradation. Mucoadhesive buccal patches are dosage forms that deliver drug at longer duration of time in controlled release manner .Moreover rapid onset of action and at the same time altering thickness and type of polymer with variety of drugs, drug release can be made faster or slower as per need. Buccal patches are dosage forms that are novel but simple dosage forms to deliver drugs also drug release can be terminated at any time by removing it. The major emphasis is given on Mucoadhesion so as to prevent accidental swallowing of drug; various combinations of polymers, permeation enhancers are used in this dosage form to enhance its efficiency. Many studies conducted relating to mucoadhesive drug delivery systems e.g. adhesive tablets, adhesive gels, adhesive patches and many more to achieve controlled or slow release delivery systems for systemic and local therapy of diseases in the oral cavity.

Development, In-Vitro and Ex-Vivo Evaluation of Muco-adhesive Buccal patches of Candesartan cilexetil

Candesartan cilexetil (CC), is an anti-hypertensive drug belongs to angiotensin-II receptor antagonist. CC possesses poor oral bioavailability due to first-pass metabolism and poor aqueous solubility. Various approaches are known to reduce the problems of first-pass metabolism. Hence, buccal drug delivery was an approach to improve bioavailability. The present study, buccal muco-adhesive patches were prepared by using hydroxyl propyl methyl cellulose (HPMC E15) and eudragit RLPO and evaluate for physicochemical properties, such as thickness, weight uniformity, folding endurance, drug content, surface pH, swelling index, moisture absorption and ex vivo permeation studies. Among all the formulations, F7 was selected as an optimized formulation and was found to be 100.55% of drug in 6 hrs, and exhibited controlled drug release, follows zero-order kinetics with diffusion as a release mechanism. The ex-vivo permeation studies revealed that 100% of drug permeated in 6 hrs. Therefore, the buccal patches of CC were successfully developed and enhancement in oral bioavailability is further confirmed by conducting in-vivo studies.

Effect of Polyox and Gum Karaya on The Release Kinetics of A Model Antihypertensive Drug From A Cellulose Derivative Based Buccal Patch

Effect of Polyox and Gum Karaya on The Release Kinetics of A Model Antihypertensive Drug From A Cellulose Derivative Based Buccal Patch

FORMULASI DAN UJI AKTIVITAS ANTIBAKTERI PATCH BUKAL MUKOADHESIF ESTRAK CENGKEH (Syzygium aromaticum L.) DENGAN KOMBINASI POLIMER POLIVINIL PIROLIDON (PVP) DAN NATRIUM KARBOKSIMETIL SELULOSA (NA-CMC) TERHADAP BAKTERI Streptococcus mutans

Clove extract ( Syzygium aromaticum ) contains eugenol 70% - 85%. The clove extract is formulated in the form of mucoadhesive buccal patches. The purpose of this study was to obtain the formulation for mucoadhesive buccal patches having optimal stability that has good pharmaceutic properties and also effectively inhibits the Streptococcus mutans bacteria. The research design used was laboratory experimental research. The mucoadhesive buccal patches with a combination of PVP and HPMC polymers made in 5 formulas based on their concentration, formula 1 1% Na-CMC concentration, formula 2 2% Na-CMC concentration, formula 3 2% PVP concentration, formula 4 3% PVP concentration, formula 5 combination of Na-CMC and PVP with concentrations of 1% and 2%. Patches obtained were tested for physical properties including organoleptic examination, surface tension, weight uniformity, thickness uniformity, folding endurance and pH patch surface. The patch is also tested for its antimicrobial power by measuring the zone of bacterial resistance. The results showed that the buccal patches of clove extract produced a dark brown color with opaque transparency, smooth surface texture with a patch weight of around 66.67 mg - 140.67 mg, standard deviation of patch thickness around ± 0.009 - ± 0.058, folding endurance more than 300 times, surface pH ranged from 6.40 - 6.60, and antimicrobial activity shows that all patch formulations can inhibit the growth of Streptococcus mutans bacteria to prevent dental caries, but the formula that has the largest inhibition zone was formula IV with a inhibition zone of about 1.667 cm.

FORMULASI DAN UJI AKTIVITAS ANTIBAKTERI PATCH BUKAL MUKOADHESIF ESTRAK CENGKEH (Syzygium aromaticum L.) DENGAN KOMBINASI POLIMER POLIVINIL PIROLIDON (PVP) DAN NATRIUM KARBOKSIMETIL SELULOSA (NA-CMC) TERHADAP BAKTERI Streptococcus mutans

Clove extract ( Syzygium aromaticum ) contains eugenol 70% - 85%. The clove extract is formulated in the form of mucoadhesive buccal patches. The purpose of this study was to obtain the formulation for mucoadhesive buccal patches having optimal stability that has good pharmaceutic properties and also effectively inhibits the Streptococcus mutans bacteria. The research design used was laboratory experimental research. The mucoadhesive buccal patches with a combination of PVP and HPMC polymers made in 5 formulas based on their concentration, formula 1 1% Na-CMC concentration, formula 2 2% Na-CMC concentration, formula 3 2% PVP concentration, formula 4 3% PVP concentration, formula 5 combination of Na-CMC and PVP with concentrations of 1% and 2%. Patches obtained were tested for physical properties including organoleptic examination, surface tension, weight uniformity, thickness uniformity, folding endurance and pH patch surface. The patch is also tested for its antimicrobial power by measuring the zone of bacterial resistance. The results showed that the buccal patches of clove extract produced a dark brown color with opaque transparency, smooth surface texture with a patch weight of around 66.67 mg - 140.67 mg, standard deviation of patch thickness around ± 0.009 - ± 0.058, folding endurance more than 300 times, surface pH ranged from 6.40 - 6.60, and antimicrobial activity shows that all patch formulations can inhibit the growth of Streptococcus mutans bacteria to prevent dental caries, but the formula that has the largest inhibition zone was formula IV with a inhibition zone of about 1.667 cm.

Prevalence of oral mucosal changes in type 2 diabetic patients attending diabetes mellitus center in Sulaimani city

Objective: Find the prevalence of possible changes seen in the oral mucosa of type 2 diabetes mellitus patients.
 Methods: Three hundred type 2 DM patients included in this study after taking their medical history and glycemic control level. Patients were asked for symptoms of dry mouth, burning sensation, pain and paresthesia and they were subjected to full oral mucosal examination. 
 Results: Most patients had one or more subjective oral complain (83%). The predominant symptom was the feeling of dry mouth (80%) with no sex difference (P= 0.772). The mucosal pain reported in (12.7%) and significantly in males (P= 0.000). Gingival redness reported in (33.3%) and paresthesia in (8%). Nine (3%) patients had white buccal patches and six of them revealed lichenoid drug reaction. Dry mouth and oral burning sensation were shown to be unrelated to the glycemic control. Gingival redness was the most common lesion and correlated with poor glycemic control. Tongue was the second most commonly affected site in both sexes; however, the type of changes was sex and age-dependent. Denture stomatitis was seen in 4% and more frequent in females and in old age patients but did not relate to glycemic status. Lichenoid drug reaction was more prevalent among patients with poor glycemic control (6.3%) and who were above 50 years old. Buccal mucosal white patches were related to the glycemic control (P = 0.014).
 Conclusions: Dry mouth was the most common complaints of a diabetic patient in all levels of glycemic control. Gingival redness was frequent in diabetic patients and correlated with poor glycemic control. Buccal white patches were more prevalent in patients with poor glycemic control and who were above 50 years old.

FORMUALTION AND DEVELOPMENT OF MUCOADHESIVE SUSTAINED RELEASE BUCCAL TABLETS AND PATCHES OF 5-FLUOROURACIL USING DIFFERENT POLYMERS

Objective: The present research study was undertaken to formulate mucoadhesive sustained release buccal tablets and patches of 5-fluorouracil (5-FU).Method: For the research experiment work design expert software version 10, stat-ease, Inc. has been used. A 32 full factorial design was selected for the formulation of the buccal tablet as well as buccal patches. In this research work, formulated tablets and patches using different polymers such as carbopol 974p, polyvinylpyrrolidone-K 30, sodium deoxycholate, microcrystalline cellulose, and polyvinyl alcohol. An after formulation of batches formulated products studied for characterization, namely, Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). Evaluation parameters studied such as weight uniformity, thickness, hardness, friability, and content uniformity also carried out. For drug release purpose from the formulation of buccal tablet and patches in vitro drug released performed. In vivo drug releases study also carried out using Rabbit for drug reaction point of view.Results: Design expert showed the significant results on independent and dependent variables. The R-Squared 0.9943 for drug release and 0.9985 for swelling index is in reasonable agreement with the formulations. FTIR and DSC indicating compatibility of the drug and polymers in the tablet formulation and patch formulations at the molecular level. The drug release of buccal tablet showed 75.10–99.34% and buccal patches showed 58.41–81.43%. These formulations showed good results when compared to the conventional tablet.Conclusion: Formulation of mucoadhesive sustained release buccal tablets and patches of 5-FU successfully done using different polymers, which would definitely help in increasing bioavailability of the drug.

Curcumin Intra-oral Controlled Release Films for Oral Candidiasis: A Comparative Study with Fluconazole, Elucidation of Release Mechanism

Objective: This research work aimed to develop bucco-adhesive patches, which release curcumin in the oral cavity for an extended duration thereby assisting in the cure of oral thrush (candidiasis). Fluconazole containing patches were also developed in order to compare the effectiveness of curcumin patches against Candida albicans. Method: After suitable preformulation studies, five formulations of curcumin were prepared using Eudragit S100 and polyvinyl alcohol (PVA) in varying ratios. Three batches of fluconazole formulations were prepared without PVA. Patches were evaluated for their physical properties and chemical integrity. Newer techniques were developed to determine their bioadhesion and tensile strength. Sterile formulations of P3 and F2 were prepared and compared for the antifungal activity against C. albicans, by zone of inhibition method. Results: All formulations exhibited satisfactory tensile strength ranging from 0.282 to 0.411 Kg/m2 with good folding endurance. Formulations containing higher amount of PVP exhibited better bioadhesive strength. P3 formulation containing curcumin and F2 formulation of fluconazole were found to sustain the drug release upto 5 hours. An increasing amount of PVA retarded the drug release. In antifungal studies, the zone of inhibition for P3 patches was 19mm, and for F2 patches, it was 13mm, indicating a better in vitro antifungal activity for curcumin against fluconazole. SEM analysis of P3 formulations revealed continuous, non-porous but non homogenous structure of the polymer film. Conclusion: The effectiveness of curcumin buccal patches in superior to fluconazole patches was well demonstrated. Mathematical modelling of drug release data indicated a first order anomalous transport causing the drug release. Kinetic modelling with zero, first order, Higuchi and Korsmeyer- peppas are explained in this article. Keywords: Buccal, curcumin, candidiasis, antifungal, tensile strength, drug release, korsmeyer-peppas.

FORMULATION AND EVALUATION OF ALGINATE-BASED MUCOADHESIVE BUCCAL PATCH FOR DELIVERY OF ANTIMIGRAINE DRUG

Objective: The present work was aimed with enhancement of oral bioavailability of sumatriptan succinate by sodium alginate-based mucoadhesive buccal patches.Methods: These patches were prepared by solvent-casting method using different concentrations of sodium alginate along with HPMC 5cps and maltodextrin as a film-forming polymer. Propylene glycol, sodium lauryl sulfate, and mannitol were used as plasticizer, penetration enhancer, and filler, respectively. Prepared patches were evaluated with respect to various in vitro parameters and in vivo studies were conducted on white strain New Zealand rabbits of either sex with average weight 2–3 kg.Results: All the formulations were transparent and homogeneous. F7 formulation containing Na alginate (250 mg), maltodextrin (250 mg), and HPMC 5cps (250 mg) displayed maximum folding endurance, mucoadhesive force, in vitro drug transport, and drug release and found to be stable up to 2 months in storage conditions. The pharmacokinetic parameters such as Cmax, tmax, and AUC were calculated from the data collected after in vivo studies. Sumatriptan succinate containing buccal patch displayed almost 1.73 folds and 2 folds higher Cmax and AUC, respectively, than plain drug solution. 1.93% of relative bioavailability was reported with the formulation.Conclusion: The outcome of the present work reveals that sumatriptan succinate-based mucoadhesive buccal formulation can improve overall performance of drug molecule in vitro and in vivo.

DESIGN AND EVALUATION OF BUCCAL PATCHES CONTAINING COMBINATION OF HYDROCHLOROTHIAZIDE AND ATENOLOL

Objective: Buccal patch is a non-dissolving thin matrix modified release dosage form which was developed to administer into the unconscious and less co-operative patients.Methods: The mucoadhesive buccal patches of hydrochlorothiazide (HCZ) and atenolol (ATN) were prepared by solvent casting technique using various concentrations of sodium alginate, hydroxyl propyl methyl cellulose, carbopol 934P and sodium carboxy methyl cellulose polymer and polyvinyl alcohol as a backing layer. The formulated patches were evaluated for their physicochemical parameters like thickness, weight variation, surface pH, content uniformity, folding endurance, swelling percentage studies and tensile strength, in vitro and ex vivo drug permeation. Results: The infra-red (IR) spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory and well within the range. Swelling of the films were increased with the increasing content of the polymers and it was found that swelling front erosion was comparably slower in the formulations with the carbopol 934 and HPMC. This is probably due to their marked viscous properties and therefore formulation provided sustained release of the drug. The percentage drug content of all the formulations were found to be in the range of 97-99 %. Among the patches, FC (Carbopol 934 and HPMC) patches were considered satisfactory for maintaining the in vitro residence in the oral cavity for almost 8h. Formulations FD (with CP and NaCMC) and FC showed high tensile strength and % E/B which is an indication of the strength and elasticity of the patch. The films were exhibited sustained release for more than 6 h which was confirmed by the in vitro release data and kinetic data reveals the combination of diffusion and erosion mechanism. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation FC.Conclusion: The formulation of HCZ and ATN mucoadhesive buccal patch was found to be satisfactory and reasonable.

SODIUM CROMOGLYCATE MUCOADHESIVE BUCCAL PATCHES: DESIGN, FABRICATION, IN VITRO AND IN VIVO CHARACTERIZATION

Objective: The purpose of this study was to design and formulate mucoadhesive buccal patches of sodium cromoglycate (SCG) as an alternative way to overcome its poor oral absorption and short half-life.Methods: Mucoadhesive patches were prepared by solvent casting technique using cellulose acetate butyrate (CAB) alone or in combination with mucoadhesive polymers like SCMC (sodium carboxymethyl cellulose), HPMC 100M (hydroxyl propyl methyl cellulose) and Cbp934P (carbopol) in different concentrations. The successful patches were evaluated for thickness, weight variation, folding endurance, tensile strength, drug content, surface pH, moisture uptake, swelling percentage, mucoadhesion strength, residence time, in vitro release study, ex vivo permeation and in vivo pharmacokinetic studies.Results: The thickness of all prepared patches ranged from 0.210±0.006 to0.355±0.012, folding endurance was more than 300, weight variation did not exceed 0.179±0.015, tensile strength and % elongation ranged from 6.4±0.018 to 13.1±0.024, and from 30.4±0.88 to 53.4±0.78respectively. The swelling percentage after one hour was from 20.8±0.99 to 53.2±1.5. pH of all prepared patches did not exceed 6.8, the drug content was about 99 to 101%, moisture uptake did not exceed 10%. Mucoadhesion strength and residence time ranged from 17.2±0.14 to 51.2±0.26, and from 3.35±0.25 to 7.45±0.28 respectively. The cumulative release percentage of SCG was in the following descending order CAB>CAB with Cbp934P>CAB with HPMC>CAB with SCMC. The optimized patch (F9) decreased the Cmax and increased Tmax compared to the parenteral solution.Conclusion: It can be concluded that mucoadhesive buccal patch is a promising dosage form to prolong the release of SCG and enhance its poor oral bioavailability.

PREPARATION AND CHARACTERIZATION OF POLY (VINYL ALCOHOL)–POLY (VINYL PYRROLIDONE) MUCOADHESIVE BUCCAL PATCHES FOR DELIVERY OF LIDOCAINE HCL

Objective: The objectives of this study were to prepare and characterize a buccal mucoadhesive patch using poly (vinyl alcohol) (PVA), poly (vinyl pyrrolidone) (PVP) as a mucoadhesive matrix, Eudragit S100 as a backing layer, and lidocaine HCl as a model drug.Methods: Lidocaine HCl buccal patches were prepared using double casting technique. Molecular interactions in the polymer matrices were studied using attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry. Mechanical and mucoadhesive properties were measured using texture analyzer. In vitro permeation of lidocaine HCl from the patch was conducted using Franz diffusion cell.Results: Both of the free and lidocaine HCl patches were smooth and transparent, with good flexibility and strength. ATR-FTIR, DSC and X-ray diffractometry studies confirmed the interaction of PVA and PVP. Mechanical properties of matrices containing 60% PVP were significantly lower than those containing 20% PVP (*P<0.05). Mucoadhesive properties had a tendency to decrease with the concentration of PVP in the patch. The patch containing 60% PVP had significantly lower muco-adhesiveness than those containing 20% PVP (*P<0.05). In vitro permeation revealed that the pattern of lidocaine HCl permeation started with an initial fast permeation, followed by a slower permeation rate. The initial permeation fluxes follow the zero-order model of which rate was not affected by the PVP concentrations in the PVA/PVP matrix.Conclusion: Mucoadhesive buccal patches fabricated with PVA/PVP were successfully prepared. Incorporation of PVP in PVA/PVP matrix affected the strength of polymeric matrix and mucoadhesive property of patches.

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCH OF TIMOLOL MALEATE

The oral transmucosal Timolol maleate delivery bypasses liver and avoids presystemic elimination in the gastro intestinal tract andliver which enhance the bioavailability as well decreases the adverse effect. Objective: The present investigation highlights the formulation andevaluation of mucoadhesive buccal patch of Timolol maleate because Timolol maleate has biphasic solubility hence relatively permeated throughbuccal mucosa, which is well supplied with both vascular and lymphatic drainage. Material and Method: The mucoadhesive buccal patches ofTimolol maleate were prepared by solvent casting technique using polymers like Hydroxypropylmethyl cellulose-15cps and Polyvinylpyrrolidone. The formulated films were evaluated for their physiochemical parameters like surface pH, percentage moisture absorption, swellingpercentage, thickness, folding endurance and drug content. In vitro permeation and in vitro release studies were performed with pH 6.8 phosphatebuffer solution. Result and Discussion: The patches exhibited controlled release for more than 12 h. The in vitro release data were fit to differentequations and kinetic models to explain release profiles. The kinetic models used were zero order, first order higuchi’s and peppa’s. The bestmucoadhesive performance and matrix controlled release was exhibited by the formulation CK2 (3 % HPMC and 1 % PVP). Conclusion: Goodresults were obtained both in physico chemical characteristics and in vitro studies in formulation CK2. Hence the formulations of Timololmaleate bioadhesive buccal patch is a promising one as the controlled drug delivery with improved bioavailability.

Formulation and Evaluation of Fexofenadine Buccal Mucoadhesive Patches

Mucoadhesive buccal patches for the delivery of fexofenadine using various polyvinyl alcohol, hydroxypropyl methyl cellulose K4M and K15M and Eudragit L100 were developed using solvent casting technique. The fabricated formulations were evaluated for different physicochemical as well as mechanical parameters such as thickness, surface pH, weight uniformity, swelling index, folding endurance, drug content, percentage moisture loss, in vitro dispersion and in vitro residence time. An in vitro drug release study was designed and performed using freshly prepared egg membrane as semi-permeable membrane. The optimized formulation (F1) showed maximum percentage of drug release 96.18% ± 0.53% by the end of 8 h. The sustained release of the drug was achieved up to 8 h.