Buccal Patches Research Articles

Development and Optimization of Curcumin and Lycopene Mucoadhesive Buccal Patches Using Response Surface Methodology

Development and Optimization of Curcumin and Lycopene Mucoadhesive Buccal Patches Using Response Surface Methodology

DEVELOPING AND ASSESSING BUCCAL PATCHES WITH ANTI-DIABETIC DRUG

DEVELOPING AND ASSESSING BUCCAL PATCHES WITH ANTI-DIABETIC DRUG

A review: Treatment of gingivitis by buccal patches

Most of the population are affected by prevalent diseases which affect the oral cavity mostly inflamed gums every now and then. Several diseases can affect the mouth, such as oral cancer, dental caries, Lichen Planus and, of course, periodontal disease with its variants. This review discusses gingivitis, a gum inflammation usually doesn’t cause any major problems at first but when left untreated it may lead to tooth damage. Later it may spread to other parts of the oral cavity, the term periodontitis is nothing but the inflammation in the periodontium the soft tissue and bone which is responsible to keep our tooth firm. As the time precedes, this periodontitis. May lead to loosen the teeth. This article also discusses the usage of buccal patches a novel delivery route for the treatment of red, swollen and bleeding gums of gingivitis.

Mucoadhesive chitosan-methylcellulose oral patches for the treatment of local mouth bacterial infections.

Mucoadhesive buccal patches are dosage forms promising for successful drug delivery. They show the distinctive advantages of long residence time on the oral mucosa and increased in situ drug bioavailability. In this context, electrophoretic deposition (EPD) of chitosan (CS) has been demonstrated as a simple and easily tunable technique to produce mucoadhesive buccal patches. However, CS-based buccal patches may suffer from weak mucoadhesion, which can impair their therapeutic effect. In this work, methylcellulose (MC), a widely investigated biopolymer in the biomedical area, was exploited to increase the mucoadhesive characteristic of pristine CS patches. CS-MC patches were obtained in a one-pot process via EPD, and the possibility of incorporating gentamicin sulfate (GS) as a model of a broad-spectrum antibiotic in the so-obtained patches was investigated. The resulting CS-MC patches showed high stability in a water environment and superior mucoadhesive characteristic (σadh = 0.85 ± 0.26 kPa, Wadh = 1192.28 ± 602.36 Pa mm) when compared with the CS control samples (σadh = 0.42 ± 0.22 kPa, Wadh = 343.13 ± 268.89 Pa mm), due to both the control of the patch porosity and the bioadhesive nature of MC. Furthermore, GS-loaded patches showed no in vitro cytotoxic effects by challenging L929 cells with material extracts and noteworthy antibacterial activity on both Gram-positive and Gram-negative bacterial strains.

Drug-loaded mucoadhesive microneedle patch for the treatment of oral submucous fibrosis.

Oral submucous fibrosis is a chronic, inflammatory and potentially malignant oral disease. Local delivery of triamcinolone to lesion site is a commonly used therapy. The existing methods for local drug delivery include topical administration and submucosal injection. However, in the wet and dynamic oral microenvironment, these methods have drawbacks such as limited drug delivery efficiency and injection pain. Therefore, it is urgently needed to develop an alternative local drug delivery system with high efficiency and painlessness. Inspired by the structure of band-aid, this study proposed a novel double-layered mucoadhesive microneedle patch for transmucosal drug delivery. The patch consisted of a mucoadhesive silk fibroin/tannic acid top-layer and a silk fibroin microneedle under-layer. When applying the annealing condition for the medium content of β-sheets of silk fibroin, the microneedles in under-layer displayed both superior morphology and mechanical property. The mechanical strength of per needle (0.071N) was sufficient to penetrate the oral mucosa. Sequentially, the gelation efficiency of silk fibroin and tannic acid in top-layer was maximized as the weight ratio of tannic acid to silk fibroin reached 5:1. Moreover, in vitro results demonstrated the double-layered patch possessed undetectable cytotoxicity. The sustained release of triamcinolone was observed from the double-layered patch for at least 7days. Furthermore, compared with other commercial buccal patches, the double-layered patch exhibited an enhanced wet adhesion strength of 37.74kPa. In addition, ex vivo mucosal tissue penetration experiment confirmed that the double-layered patch could reach the lamina propria, ensuring effective drug delivery to the lesion site of oral submucous fibrosis. These results illustrate the promising potential of the drug-loaded mucoadhesive microneedle patch for the treatment of oral submucous fibrosis.

Formulation and Characterization of Buccal Patches of Oxaceprol

Background: Oxaceprol is an anti-inflammatory and antirheumatic agent. Buccal route has advantage over conventional mode of drug administration. It avoids hepatic first pass metabolism and improve patient compliance. The main objective of the present study is to formulate and evaluation of buccal patches of Oxaceprol to overcome drawbacks of conventional dosage forms. Buccal patches were prepared by solvent-casting method using HPMC K-15 and PEG as plasticizer. Oxaceprol was initially characterized for its preliminary studies such as organoleptic properties, melting point, solubility, UV Spectroscopy, and FTIR studies. Drug-excipients compatibility was confirmed by FTIR, DSC and assay of drug content. The formulations were prepared and evaluated for parameters like physical appearance, thickness, weight uniformity, % moisture loss, folding endurance, drug content uniformity. All prepared patches of drug were smooth and elegant in appearance. No visible cracks were observed. All formulations were uniform in weight, thickness, and drug content. The folding endurance was increased with an increased in polymer concentration. In vitro drug release of F6 batch was 93.78% at the end 8 hr. Oxaceprol buccal patches showed enhanced the bioavailability. Release exponent n value obtained from Kors Meyer- Peppa’s equation was within 0.5 -1.0 which indicates anomalous release.

Studies on Formulation and Evaluation of Buccal Patch for Delivery of an Anti-Hypertensive Drug

Studies on Formulation and Evaluation of Buccal Patch for Delivery of an Anti-Hypertensive Drug

The effect of vitamin C in the formulation of pectin/thiolated alginate buccal adhesive patches: In vitro and Ex vivo evaluation

The present study outlines the prospect of a pectin (Pec)/modified alginate (Alg) buccal patch as drug delivery device in the localized treatment of oral cavity diseases. Firstly, Alg was modified with acrylic acid, and thiolated with cystein to enhance its mucoadhesive properties. Then modified Alg was characterized with Fourier transform infrared (FTIR) and proton nuclear magnetic resonance (1HNMR) spectroscopy. As a proof of concept, Pec/modified Alg buccal patches were formed via the conventional solvent casting technique. Then the patches were characterized by FTIR and differential scanning calorimetry/thermal gravimetric analysis (DSC/TGA). Vitamin C (Vit C) was used for in vitro drug release assay, and the release amount was 2.10 mg/g polymer in simulated salivary pH 6.8. Ex vivo mucoadhesion assays of Vit C loaded Pec/modified Alg patch did not have a negative effect on the mucoadhesion feature of the material. The cytotoxicity study indicated that Pec/modified Alg buccal patches did not exhibit apparent cytotoxicity against NIH/3T3 cell lines. Notably, it was found that Vit C in the patch formulation has an accelerating effect on wound healing. According to all results, Vit C loaded Pec/modified Alg buccal patch might be a promising candidate for localized buccal drug release systems.

Development of Fast Dissolving Buccal Patches of Prochlorperazine Maleate for Effective Management of Emesis

The goal of this research was to increase the oral bioavailability and avoid the first pass metabolism of Prochlorperazine Maleate (used to treat nausea and vomiting) by creating its buccal patches. Prochlorperazine is a member of BCS II and has an oral bioavailability of 11– 15%. Prochlorperazine maleate buccal patches were made by solvent casting with the aid of HPMC E-15 and Chitosan (film-forming agents), Glycerol (plasticizer), Tween 80 (penetration enhancer), Citric Acid (saliva stimulating agent), Mannitol (sweetening agent), and Ethyl Cellulose (Backing membrane). Twelve total formulations was made by using different quantities of polymers and formulation was evaluated for weight variation, thickness, folding endurance, drug content, in- vitro diffusion, in vitro, bio-adhesion time, percent moisture loss, % swelling index and stability study. Based on results it was concluded that buccal patches (F4) showed enhanced bioavailability. Keywords: Prochlorperazine maleate, Buccal Patches, Bioavailability, Stability

SEDDS-loaded mucoadhesive fiber patches for advanced oromucosal delivery of poorly soluble drugs.

To date, buccal administration of lipophilic drugs is still a major challenge due to their poor solubility in saliva and limited penetration into mucosal tissues. To overcome these limitations, we developed electrospun patches combining the benefits of mucoadhesive fibers and self-emulsifying drug delivery systems (SEDDS). The fiber system comprises a combination of mucoadhesive thiolated polyacrylic acid fibers and SEDDS-loaded fibers fabricated by parallel electrospinning. The resulting mucoadhesive electrospun SEDDS patches were systemically investigated for fiber characteristics, self-emulsification, mucoadhesion, drug penetration into porcine buccal tissue and biocompatibility. The patches showed high encapsulation efficiency for SEDDS without causing fiber defects or leakage. SEDDS incorporation enhanced the spinning process and reduced the fiber diameter and fiber size distribution. Hydration-dependent self-emulsification provided a controlled release of curcumin being encapsulated in nano-scaled o/w emulsion for over 3h. Due to the thiolated polyacrylic acid fibers, the buccal residence time of patches was 200-fold prolonged. Further, they promoted a significantly increased drug penetration into buccal tissue compared to fiber patches without SEDDS. Finally, biocompatibility and improved therapeutic effects of curcumin-loaded patches on human keratinocytes and fibroblasts were confirmed. Mucoadhesive electrospun SEDDS patches represent a promising approach to overcome current challenges in the oromucosal delivery of lipophilic drugs to unlock their full therapeutic potential.

Development and Evaluation of Polymer Drug Delivery System (PDDS) for Delivery of Boswellia seratta

Boswellia seratta (BS) is the best herbal medicine to treat Rheumatoid Arthritis (RA), due to its anti-inflammatory and anti-arthritic activity. Delivering BS through an oral drug delivery system has been in effective, because of its enzymatic degradation within the Gastro-Intestinal (GI) tract. In this paper, we develop a gastro retentive approach for delivering BS to avoid high hepatic first pass metabolism and optimized buccal patch based on the drug delivery characteristics. There are seven different formulated buccal films of BS that were prepared by the solvent casting method, using mucoadhesive polymers, Poly Vinyl Alcohol (PVA), and Sodium Carboxy Methyl Cellulose (SCMC). These with drug formulation can be represented as PCB. The prepared films were evaluated by various physicochemical properties and characterization studies. Results obtained from physico-chemical properties, in-vitro and ex-vivo studies among all seven patches, PCB5 shows better drug-releasing characteristics. This was further confirmed by FT-IR and XRD characterization studies. Also, the data was statistically analysed using Analysis of Variance (ANOVA).

Buccal drug delivery system

It is well known that certain medications suffer hepatic first-pass metabolism or deteriorate in the digestive system, the buccal drug delivery method may be an alternative to oral administration. Because it is painless and may be swiftly and readily removed if the treatment must be terminated or interrupted, the buccal mucosa has long been ideal for administering medications. This paper focuses on the buccal drug delivery system had the goal of gathering recent literature and presenting a concise explanation of buccal patches by discussing the characteristics of an ideal mucoadhesive system, benefits of buccal delivery and disadvantages thereof, factors affecting buccal absorption, and various types of patches as well as the preparation method and composition thereof. The compilation of the data is also enhanced by adding market products as well as the patented, so that reader will get the complete knowledge about the buccal drug delivery.

The effect of thiol functional groups on bovine serum albumin/chitosan buccal mucoadhesive patches

In this research, the effect of thiol functional groups on bovine serum albumin (BSA)/chitosan (Chi) based buccal mucoadhesive patch was investigated. Thiolated BSA (BSA-SH) was prepared via 2-mercaptoethanol. FTIR and 1H NMR results confirmed that BSA-SH was synthesized successfully. The buccal mucoadhesive patches were fabricated by the solvent casting method. Following the structural characterization of BSA/Chi and BSA-SH/Chi buccal patches, the mechanical characterization was performed by tensile tests. The drug release from triamcinolone acetonide (TR) loaded buccal patches was evaluated in-vitro in simulated salivary. According to the ex-vivo buccal adhesion experiments, the mechanical and mucoadhesion properties of BSA-SH/Chi buccal patch had improved compared to BSA/Chi buccal patch. The total cumulative TR permeated after 12 h was higher for BSA-SH/Chi than BSA/Chi buccal patches. The developed mucoadhesive buccal patches were found to be biocompatible in vitro. To conclude, the thiolated BSA-SH/Chi buccal adhesive patch is a promising biomaterial for a satisfied drug delivery, which provides advantages for various oral applications.

Critical review on buccal mucoadhesive drug delivery systems

Traditional oral dosage forms prone to first pass metabolism and degra­dation due to enzymes but mucoadhesive dosage form able to bypass first pass metabolism and related degradation. It also offers more patient compliance without risk of chocking in case of paediatric and geriatric patients. Buccal mucosa is considered as a convenient and easily accessible site for the drug administration for both local and systemic delivery. Mucoadhesion is a process involving chemical interactions between mucin and polymers. The use of mucoadhesive polymers in buccal drug delivery has gained a great attention. Various mucoadhesive dosage forms, including tablets, patches, disks, wafers, ointments and gels have recently been developed. Amongst them, buccal patches offer greater flexibility and comfort than the other forms. Smart materials such as stimuli-responsive hydrogels, liposome-based patches, polymeric micelles, etc. play a vital role in the development of these drug delivery systems by their efficient carrier capacity, prolonging the residence time of the drug at the site of absorption, improved drug bioavailability, reduced dosing frequency and improved patience compliance.

DEVELOPMENT EVALUATION AND CHARACTERIZATION OF BUCCAL PATCHES CONTAINING ATENOLOL USING HYDROPHILIC POLYMERS

Objective: The present investigation focused on fabrication and evaluation of atenolol releasing buccal patches comprising mucoadhesive hydrophilic polymers like sodium alginate and tamarind seed polysaccharide with a drug-free backing layer (6 % ethylcellulose). Methods: Solvent evaporation technique being employed in the development of atenolol comprising buccal patches using mucoadhesive hydrophilic polymers. The prepared buccal patch formulations were tested for thickness, weight variation, folding endurance, drug content, moisture content, moisture absorption, % swelling, surface pH, in vitro residence time and mucoadhesion studies. The drug permeation through goat buccal mucosal membrane was conducted with the use of Franz diffusion cell in phosphate buffer saline, pH 6.8 and was subjected to FT-IR and SEM characterization. Stability study was performed as per ICH guidelines. Results: For all the buccal patch formulations, the average weight, thickness, drug content, moisture content, moisture absorption, % swelling, surface pH study exhibited satisfactory results. Out of 7 different buccal patches, the formulation FA-1 revealed the highest mucoadhesive strength (31.36±0.95 g), the force of adhesion (0.31±0.04 N), maximum swelling index (341±0.83 %) and more than 24 h in vitro residence time. The buccal patch formulation FA-1 indicated highest drug permeation (97.51 %) in 24 h and was found to be stable. FT-IR examination confirms lack of drug polymer interaction. SEM investigation reveals a smooth surface of the buccal patch. Conclusion: The developed buccal patches comprising atenolol can be very promising in increasing patient compliance and reducing dosing frequency.

Polymeric and electrospun patches for drug delivery through buccal route: Formulation and biointerface evaluation

IntroductionOf the various transmucosal routes which are being considered for extended and controlled drug delivery, buccal route is superior to other methods owing to high administrability and milder environment for drug absorption. In this direction, mucoadhesive buccal films of venlafaxine were fabricated using a combination of biocompatible polymers. AimThe main objective of the study was to standardize an optimized formulation of polyvinyl alcohol, sodium carboxymethyl cellulose and sodium alginate that would lead to sustained drug delivery in the form of buccal patches. MethodsVarying polymeric concentrations were utilized for the fabrication of buccal patches via solvent casting method. The physical parameters were evaluated, followed by in vitro drug release studies. The electrospun nanofibers were prepared for optimized formulations and the buccal delivery system was compared to oral and intravenous routes for absorption, distribution, and elimination during in vivo studies using venlaflaxine. ResultsThe patches had high tensile strength with uniform drug content and surface pH in the range of 6.28–6.88. The release of drug was steady witha maximum release of 89.97% at 5 h. The negative hemolytic and cytotoxicity studies with TR146 cells over a range of concentrations indicated biocompatibility of the mucoadhesive patch with human tissues. The pharmacokinetics of the buccal patch of the radiolabeled drug, 99mTc-venlaflaxine, displayed favorable release pattern. The radiolabeled patch attached to rabbit buccal mucosa displayed high retention with controlled drug release as indicated by the Cmax and T1/2 values (19.94 ng/ml and 3 h). The drug release mechanism corresponded to a pure fickian diffusion-controlled mechanism following Higuchi's model. Electrospun fibrous patch of the drug had a 10% higher drug release than solvent cast patch. ConclusionIn vitro and in vivo data indicate that the polymeric system was successfully optimized for sustained drug release for about 5 h in a continuous manner with electrospun fibrous patch showing 10% increase in drug release studies. The patches displayed ideal physical and biocompatibility characteristics. This polymeric combination can therefore be further utilized for development of novel drug delivery systems with sustained drug release pattern.

Evaluation of modified pectin/alginate buccal patches with enhanced mucoadhesive properties for drug release systems: In-vitro and ex-vivo study

A recent approach for buccal mucoadhesive system is the production of thiolated polymers via thiomer. In this study, pectin was grafted with acrylic acid before the thiolation by L-cystein and it was characterized by FTIR, 1H NMR, and TGA. Following that, modified/unmodified pectin and alginate patches were successfully fabricated by a casting method, and they were characterized by FTIR and TGA. The modified pectin/alginate patches had a higher swelling ratio than that of unmodified pectin/alginate patches. Moreover, ex-vivo mucoadhesion studies of modified pectin/alginate buccal patch was 0.11 ± 0.033 N which meant that mucoadhesion on buccal mucosa was improved as compared to unmodified pectin/alginate buccal patch. The triamcinolone acetonide release capacity of the modified pectin/alginate and unmodified pectin/alginate patches in pH 6.8 was found to be 32.6 and 28.5 mg/g, respectively. The drug release kinetic data best fitted with Korsmeyer-Peppas model for both buccal patches. To cell culture studies, drug loaded, and unloaded buccal patches had no cytotoxicity against L929 cell line. According to our results modified pectin/alginate buccal patch can be used as a promising alternative for buccal mucoadhesive drug release systems.

Development and Evaluation of Trans Buccal Patches based on Natural and Synthetic Polymers Loaded with Rivastigmine using Solvent Casting Technique

Mucoadhesive buccal films of rivastigmine were prepared by the solvent casting technique using HPMC K15M, sodium alginate, glycerine, and Eudragit RL100. Arranged films assessed for weight variation, thickness, % drug substance, % moisture loss, % moisture take-up, folding endurance, in-vitro medicament release, and Fourier transform Infrared spectroscopy (FTIR). The films showed a controlled release (CR) over 8 h. The preparation observed to be a worthy candidate for the development of buccal patches for therapeutic purposes. Drug-polymer compatibility considers FTIR demonstrated no contradiction between the medicament and the polymers. The optimized formulation found F7 indicated drug release 85% at the end of 8 h. Thinking about the correlation coefficient (R2) values got from the kinetic equations, the drug release from the formulations F1-F8 has discovered zero-order release mechanism. It can be concluded that oral buccal patches of rivastigmine, for treatment of Alzheimer’s and Parkinson’s disease, can be formulated. The study suggests that rivastigmine can be conveniently administered orally in the form of buccal patches, with the lesser occurrence of its side effects and improved bioavailability.

Design and In-Vivo Evaluation of Risperidone Buccal Mucoadhesive Patches of Interpolymer Matrix

The buccal cavity is an alternate route for the administration of the drug. This route gained acceptance as increase in bioavailability is observed due to bypass of first pass metabolism. Solvent casting method was employed for the preparation of the risperidone mucoadhesive patches using different combinations of water soluble and water insoluble polymers using polyvinyl alcohol as a backing layer. Our main objective of this study was to understand the behaviour of water soluble and water insoluble polymers in combination on release pattern. Six different formulations of mucoadhesive patches were evaluated for physicochemical parameters like weight uniformity, content uniformity, thickness uniformity, surface pH, swelling studies, tensile strength, folding endurance, in-vitro drug release, and in-vivo drug absorption. Drug loaded mucoadhesive patches of various polymer bases had shown 35.64 to 72.33% drug release in 30 min in phosphate buffer solution of pH 6.6. In-vitro release data from patches were fit to different equations and kinetic models to explain release profiles. Kinetic models like Hixon-Crowell and Higuchi models were used. The formulation containing HPMC (15Cps) and polyvinyl pyrrolidone was considered as optimized based on the physicochemical and pharmaceutical properties. In-vivo studies in rabbits, carried out with prior permission from IAEC, showed 80.40% of drug release from the optimized patches. In-vivo and in-vitro correlations were found to be good. The drug absorption was found significant from the optimized formulation in healthy rabbits. The structure of the buccal membrane and permeability factors are similar in both human beings and rabbits. Therefore mucoadhesive patches of risperidone may be accepted with the important advantage of reduced risperidone dose.

Formulation and In Vitro/In Vivo Evaluation of Metoclopramide Mucoadhesive Buccal Patches for Effective Pain Management

The report planned to design plus valuate mucoadhesive buccal patches of Metoclopramide for orthopedic treatment of pain and inflammations. All eight formulation acquire numerous evaluation parameters, it used to be complete for which F1 confirmed good mucoadhesive strength, encouraging pressurized and arrant drug release, easiest In-vivo residence time, swelling index and pH shows the best formulation. The acquired in vivo effects show that the put concentration of Metoclopramide in the mouth cavity was retained above 5 pg/mE for 130 min. The effect stands for so the buccal patches of metoclopramide could be a good choice to avoid the unsatisfactory systemic unwanted effects and will be planned as a new therapeutic tool around against orthopedic diseases and disturbances.