Buccal Permeation Research Articles

Assessing α-Bisabolol as a Transmucosal Permeation Enhancer of Buccal Local Anesthetics.

Needle-free buccal anesthesia improves dental treatment outcomes for both patients and dentists. In this study, we report on an assessment of the enhancement effects of α-bisabolol on the in vitro transmucosal permeation of prilocaine hydrochloride (PCl) and lidocaine hydrochloride (LCl) from needleless buccal films. We also evaluated the mechanical properties of the film, which consisted of Methocel™ K100 LV as the film-forming polymer (3% m·m-1), PEG 400 as a cosolvent (15% m·m-1 based on drug loading), α-bisabolol (15 and 30% m·m-1 based on drug loading), and the drugs combined at a 1:1 ratio (15 mg·unit-1). The porcine esophageal epithelium was used as a membrane barrier, and artificial saliva was the release medium. After a 1 h experiment at 25 ± 2 °C, α-bisabolol significantly decreased, rather than enhanced, the permeation fluxes (five-fold), permeability coefficients (seven-fold), and retentions (two-fold) of both PCl and LCl through the epithelium, regardless of the concentration. Moreover, the resistance and flexibility of the films markedly decreased compared to those without α-bisabolol. Therefore, under the experimental conditions, using α-bisabolol as a buccal permeation enhancer for the hydrophilic local anesthetics PCl and LCl from buccal films is not feasible.

Evaluating the role of amino acids and isothermal dry particle coating in modulating buccal permeation of large molecule drug vancomycin

The formulation and delivery of macromolecules through the oral route pose considerable challenges due to factors such as large molecular weight, pH sensitivity, and limited formulation approaches. This challenge is compounded if the drug is poorly permeable, necessitating innovative drug delivery strategies. Vancomycin, a widely prescribed glycopeptide antibiotic, has an oral bioavailability of less than 10%, leading to predominantly intravenous administration and potential patient discomfort. This study explores the potential of the buccal route as a non-invasive, highly vascularised alternative route of administration, offering a rapid onset of action while bypassing the first-pass metabolism. In this study, vancomycin was coated with L-glutamic acid using an isothermal dry particle coater to modulate permeation through the buccal cell line, TR146. Results confirm significant impact of both amino acid concentration and dry particle coating on the rate and extent of drug permeability. With the introduction of L-glutamic acid and utilisation of the isothermal dry particle coater, vancomycin’s permeation profile increased six-fold compared to the control due to the formation of drug ion-pair complex. Imaging studies showed the presence of layered micronized glutamic acid particles on the surface of dry coated vancomycin particles which confirms the role of dry coating and amino acid concentration in modulating drug permeation. Microbiology experiments in Staphylococcus aureus, minimum inhibitory concentration and biofilm disruption studies, provided confirmatory evidence of antimicrobial activity of dry coated glutamic acid-vancomycin ion pair particulate structure. This study demonstrates, for the first-time, buccal delivery of dry coated large molecule drug, vancomycin, through controlled deposition of amino acid using innovative particle coating strategy.

Formulation Development of Medicated Chewing Gum by Direct Compression utilizing the SeDeM Diagram Expert System

The main objective of this study was to prepare and characterize the MCG of Ondan HCl which helps to improve the effectivity of the drug and to investigate the applicability of the SeDeM system for the formulation of MCG. The Ondan HCl was formulated into directly compressed MCG utilizing the SeDeM Diagram Expert System. The MCG was optimized using 32 factorial design. Performance evaluation was carried out by evaluating different parameters. Statistical analysis showed that micromeritic properties were improved after inclusion of appropriate excipient in optimum amount. In-vitro drug release study showed 90.01% drug release whereas ex vivo buccal permeation study exhibited significant drug permeation within 15 min indicating its potential for increasing bioavailability. It was concluded that various characteristics of powder material at pre formulation level can be successfully predicted by SeDeM diagram expert system. The developed medicated chewing gum is more effective than mouth dissolving and conventional tablet formulation.
 Keywords: Ondansetron HCl; Medicated chewing gum; direct compression; SeDeM diagram expert system.

Formulation and evaluation of buccal film of an antihypertensive drug

The aim of the study was to formulate and evaluate Losartan potassium buccal films, an angiotensin receptor blocker and is used to treat hypertension. Losartan potassium is having less bioavailability (33%), so the buccal films are expected to increase the bioavailability by avoiding hepatic metabolism. Ten formulations of buccal films were prepared by solvent casting method using HPMC K15 M as the main film-forming polymer in various proportions with various co-polymers such as Eudragit RL. 100, Carbopol 940, Ethyl cellulose. Physicochemical characteristics,in vitro buccal permeation, in vitro release study and residence time were evaluated. In vitro studies revealed that the release rate of Losartan potassium was higher for films containing HPMC K15 M and Eudragit RL100 in 3:1 ratio. The result of stability study indicated that no significant changes have occurredduring the period of study.

Development of a buccal in vitro permeation method – exploring aQbD implementation

The buccal mucosa is arising within the pharmaceutical landscape as an attractive option for local and systemic drug delivery, mostly due to its high vascularization, inherent permeability and robustness. Still, one of the major challenges in bringing oromucosal preparations to market remains the accurate evaluation of permeability. During pre-clinical drug development, in vitro permeation assessment is essential, and methodologies, based on the selection of a proper membrane in a diffusion cell, have become appealing alternatives to the conventional cell-based models. The development of such methods is being constrained by the number of variables - related to study conditions, setup and formulation - that need to be optimized to accurately estimate buccal permeation. The gap of knowledge over the mentioned variables may lead to long costly developments and poorly accurate methods, especially if the empirical analytical approach is used.In this paper, a systematic risk-based analytical quality by design approach was applied to the development of a buccal in vitro permeation method, ensuring that all sources of variability affecting permeation process were identified, explained and managed by appropriate measures. Researchers are guided through a step by step model, successfully demonstrating with experimental data the impact of critical variables on method’s performance.

Candesartan exhibits low intrinsic permeation capacity and affects buccal tissue viability and integrity: An ex vivo study in porcine buccal mucosa

Candesartan is a nonpeptide angiotensin II receptor blocker that selectively binds to angiotensin II receptor subtype 1. It is administered orally in its ester form (candesartan cilexetil). However, its poor aqueous solubility results in its low bioavailability; therefore, other routes of administration must be explored. The buccal mucosa has been extensively studied as an alternative route for drug delivery as it improves the bioavailability of drugs administered via the peroral route. Porcine buccal mucosa has been widely used as an ex vivo model to study the permeability of various diffusants; however, studies on candesartan are limited. This study aimed to evaluate the ex vivo permeation profile of candesartan and its effects on the viability and integrity of porcine buccal mucosa. Initially, we evaluated the viability, integrity, and barrier function of the buccal tissue before performing permeability tests using freshly excised tissues or tissues after 12 h of resection. Here, three indicators were used: caffeine, β-estradiol, and FD-20 penetration; mucosal metabolic activity, as determined using MTT reduction assay; and haematoxylin and eosin staining. Our results indicated that the porcine buccal mucosa preserved its viability, integrity, and barrier function before the permeation assay, allowing the passage of molecules with a molecular mass of less than 20 kDa, such as caffeine, but not β-estradiol and FD-20. Furthermore, we analyzed the intrinsic capacity of candesartan to diffuse through the fresh porcine buccal mucosa under two pH conditions. The concentration of candesartan in the receptor chamber of Franz diffusion cell was quantified using ultra-high liquid chromatography. In the permeation assay, candesartan exhibited a low intrinsic permeation capacity that impacted the buccal tissue viability and integrity, suggesting that using the buccal mucosa as an alternative route of administration requires developing a pharmaceutical formulation that reduces the adverse effects on mucosa and increasing the buccal permeability of candesartan.

Buccal Permeation of Polysaccharide High Molecular Weight Compounds: Effect of Chemical Permeation Enhancers.

The greatest achievement in the advanced drug delivery field should be the optimization of non-invasive formulations for the delivery of high molecular weight compounds. Peptides, proteins, and other macromolecules can have poor membrane permeation, principally due to their large molecular weight. The aim of this work was to explore the possibility of administering fluorescently labeled dextrans (molecular weight 4-150 kDa) across the buccal mucosa. Permeation experiments across pig esophageal mucosa were carried out using fatty acids and bile salts as penetration enhancers. The data obtained show that it is possible to increase or promote the mucosa permeation of high molecular weight dextrans by using caprylic acid or sodium taurocholate as the chemical enhancers. With these enhancers, dextrans with molecular weight of 70 and 150 kDa, that in passive conditions did not permeate, could cross the mucosa in detectable amounts. FD-70 and FD-150 showed comparable permeability values, despite the molecular weight difference. The results obtained in the present work suggest that the buccal administration of high molecular weight compounds is feasible.

Effect of quaternary ammonium surfactant on<em> </em>buccal permeation of budesonide film formulation: <em>in silico</em> docking studies

Budesonide, an immunosuppressant glucocorticosteroid generally used to ameliorate chronic inflammation. Low bioavailability due to first pass metabolism decreases its therapeutic activity. The present study focuses on the formulation of a biodegradable buccoadhesive film for improvement of buccalpermeation. Transparent buccoadhesive films were prepared by incorporating budesonide in HPMC matrix with triethalonamine as a plasticizer and a number of surfactants. Absence of the characteristic drug melting peak at 252°C in Differential Scanning Calorimetry (DSC) thermogram study confirmed almost complete amorphization of the drug to a homogenous solid-solid mixture in the film. The characteristic Fourier-Transform Infrared Spectroscopy (FTIR) peak of pure drug showed the carbonyl stretching in between 1600–1900 cm −1 and C–O stretching at 1095 cm −1 . Broadening of C–O stretching and masking of carbonyl stretching confirmed the drug polymer interaction. In vitro dissolution and ex-vivo buccal tissue permeation revealed upto 72% and more than 58% respectively using surfactants upto 6 hour of study. Enhanced buccal permeability and flux were found in presence of surfactant compared to its absence. New film formulation could be developed including surfactant for improved buccal permeation with expected increased bioavailability. The in silico study confirmed about a stable interaction between drug and polymer (−3.1 kcal/mol).

Feasibility of mucoadhesive chitosan maleimide-coated liposomes for improved buccal delivery of a protein drug

Chitosan-maleimide (CSMHA) coated liposomes were developed for the buccal delivery of protein. Albumin–fluorescein isothiocyanate conjugate (FITC-BSA) was used as a protein replica to be loaded in the liposomes. The liposomes were formed by a thin-film hydration technique before being decorated with CSMHA. The mucoadhesive capability of the CSMHA-coated liposomes on the porcine buccal mucosa, the loading efficiency and loading capacity, drug release, permeation through buccal mucosa, protein integrity, the cytotoxicity on oral fibroblast cells, and biocompatibility were investigated. The liposome formulations were obtained with sizes of 35–166 nm. CSMHA-coated FITC-BSA-loaded liposomes remained on the buccal tissue to the highest extent. Moreover, CSMHA-coated liposomes provided the highest buccal permeation of FITC-BSA and were safe for normal gingival fibroblast cells and buccal tissue. Therefore, the CSMHA-coated liposomes may have the capability to improve protein delivery via the buccal route.

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.

Permeability of Buccal Mucosa.

The buccal mucosa provides an alternative route of drug delivery that can be more beneficial compared to other administration routes. Although numerous studies and reviews have been published on buccal drug delivery, an extensive review of the permeability data is not available. Understanding the buccal mucosa barrier could provide insights into the approaches to effective drug delivery and optimization of dosage forms. This paper provides a review on the permeability of the buccal mucosa. The intrinsic permeability coefficients of porcine buccal mucosa were collected. Large variability was observed among the published permeability data. The permeability coefficients were then analyzed using a model involving parallel lipoidal and polar transport pathways. For the lipoidal pathway, a correlation was observed between the permeability coefficients and permeant octanol/water partition coefficients (Kow) and molecular weight (MW) in a subset of the permeability data under specific conditions. The permeability analysis suggested that the buccal permeation barrier was less lipophilic than octanol. For the polar pathway and macromolecules, a correlation was observed between the permeability coefficients and permeant MW. The hindered transport analysis suggested an effective pore radius of 1.5 to 3 nm for the buccal membrane barrier.

DEVELOPMENT AND EVALUATION OF MEDICATED CHEWING GUM OF RALOXIFENE HYDROCHLORIDE

In this study we formulate Raloxifene hydrochloride, edicated chewing gum to overcome first pass metabolism of it so bioavability increase of drug. We take polyvinyl acetate as chewing gum base. Aspartame, mannitol and sucrose as sweetener. Glycerin as a plasticizer. Beta-cyclodextrine as solubility enhancer and taste masking agent. First we evaluate the API by its melting point after we derived its calibration curve. After this we select proper ratio of Beta-cyclodextrine and API. After we study drug and excipients compatibility by using FTIR. XRD study perform for API and formulation. After we formulate our formulation and perform post-evaluation study like hardness, weight variation, % drug content and % drug release. From all formulation F5 formulation shows best % drug release and % drug content. After we perform stability study for our formulation and after study no major change show in formulation. And in last we perform buccal permeability study. On basis of all study results we can say that our formulation is successfully formed.
 Keywords: Raloxifene hydrochloride, Medicated chewing gum, Buccal permeation, Osteoporosis.

Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

Buccal drug delivery is a suitable alternative to invasive routes of drug administration. The buccal administration of insulin for the management of diabetes has received substantial attention worldwide. The main aim of this study was to develop and characterize elastic liposomes and assess their permeability across porcine buccal tissues. Sodium-cholate-incorporated elastic liposomes (SC-EL) and sodium-glycodeoxycholate-incorporated elastic liposomes (SGDC-EL) were prepared using the thin-film hydration method. The prepared liposomes were characterized and their ex vivo permeability attributes were investigated. The distribution of the SC-EL and SGDC-EL across porcine buccal tissues was evaluated using confocal laser scanning microscopy (CLSM). The SGDC-EL were the most superior nanocarriers since they significantly enhanced the permeation of insulin across porcine buccal tissues, displaying a 4.33-fold increase in the permeability coefficient compared with the insulin solution. Compared with the SC-EL, the SGDC-EL were better at facilitating insulin permeability, with a 3.70-fold increase in the permeability coefficient across porcine buccal tissue. These findings were further corroborated based on bioimaging analysis using CLSM. SGDC-ELs showed the greatest fluorescence intensity in buccal tissues, as evidenced by the greater shift of fluorescence intensity toward the inner buccal tissue over time. The fluorescence intensity ranked as follows: SGDC-EL > SC-EL > FITC–insulin solution. Conclusively, this study highlighted the potential nanocarriers for enhancing the buccal permeability of insulin.

In-vitro/in-vivo evaluation of Paclitaxel Freeze-Dried micellar nanoparticles intended for buccal delivery

Biopharmaceutics Classified drugs in the category II, III and IV encounter many challenges during development of buccal formulations with adequate bioavailability. This study took the advantage of nanoparticles based on permeability enhancers (PEs) to develop novel paclitaxel (PX) nanoparticles suitable for designing buccal tablets (BTs). Various PX-nanosuspensions were produced using selected PEs, then converted into dry-nanoparticles (PX-NPs) using Lyophilization. Dependent variables included homogenization speed, homogenization time, and PE concentration which were optimized for appropriate particle size and entrapping efficiency. Optimized buccal tablets were then evaluated for in-vitro disintegration-time (Dt), dissolution, ex-vivo permeation, and in-vivo bioavailability using rabbit models. The results were compared to pure PX powder. The Optimized formulation containing Pluronic F68 increased PX dissolution-rate (95% after 5min) and enhanced its transport through the buccal mucosal-membrane by two folds. This formulation also showed lowest PX particle size (≈250 nm). PX-NPs-based tablets containing mannitol as diluents, Avicel-PH102 as a binder, and Ac-Di-Sol as super-disintegrant demonstrate short in-vitro disintegration (Dt ≈ 36sec), and rapid release rate >70% within first minute. Moreover, PX bioavailability increased six times compared to pure PX. These findings confirm that nanoparticles featured with permeability enhancers could be an effective solution for improving buccal permeability and absorption of poorly soluble chemotherapeutic drugs intended for oral tumors.

MUCOADHESIVE POLYMERIC FILMS OF ACYCLOVIR PRONIOSOMES FOR BUCCAL ADMINISTRATION

Objective: The aim of the present work was to formulate and evaluate proniosomes of the poorly soluble drug, acyclovir incorporated in mucoadhesive polymeric films for improved buccal mucosal permeability of the drug while achieving prolonged release.
 Methods: Acyclovir was formulated as proniosomes using Span 60 and cholesterol. The prepared proniosomes were loaded into mucoadhesive polymeric films prepared with varying quantities of carbopol 934P and HPMC K15M. The proniosome incorporated films were evaluated for physicomechanical characters, mucoadhesion, swelling index, drug content, in vitro drug release and ex vivo permeation through porcine buccal mucosa.
 Results: Hydration of the proniosomes produced spherical vesicles or niosomes, which was confirmed by Scanning Electron Microscopy. The optimized formulation selected on the basis of vesicle size, entrapment efficiency PDI, Zetz potential and in vitro drug release was selected for incorporation into mucoadhesive polymeric films. All the films showed excellent physicomechanical characters. Formulations with higher proportions of carbopol produced slower in vitro drug release. The kinetics of release of drug from all the formulations appeared to be zero-order based on their regression coefficient values. Comparative evaluation of ex vivo permeation from niosomal and non-niosomal films indicated that the former demonstrated improved mucosal permeation and drug release was also sustained for the 8 h period.
 Conclusion: Mucoadhesive films impregnated with acyclovir loaded proniosomes could be a potential approach for buccal delivery of acyclovir for improving its absorption and bioavailability.

Transbuccal delivery of metal complexes of isoniazid as an alternative to overcome antimicrobial resistance problems.

In isolated isoniazid (INH)-resistant strains, deletion or mutations in thekatGgene have been identified, which result in loss of catalase-peroxidase activity. This enzyme plays a key role in the activation of this prodrug. As an alternative, the coordination of the INH to metal complexes has been purposed to activate it regardless of enzyme functionality. Although pentacyanido(isoniazid)ferrate(II) complexes have shown to be effective against resistant strains of Mycobacterium tuberculosis, low oral bioavailability was found. In this context, buccal mucosa was selected as an alternative route to the metal complex delivery. Moreover, oral manifestations of tuberculosis(TB) have been observed in some patients, particularly when resistant strains are present, and no therapeutic options are currently available on the market. Pentacyanidoferrate (PCF-INH) and Prussian-blue (PB-INH) complexes were initially prepared and characterized, followed by buccal permeability studies in Franz-type diffusion cells. The electrochemical potential of the complexes demonstrated their ability to self-activate. Job's method suggested the presence of structural defects in PB-INH complexes, which was correlated with permeability results. In fact, PB-INH showed a higher dissociation rate in salt-rich aqueous medium and thus a high transport rate of INH through the buccal mucosa. Its passage through the tissue would not be possible due to the high molecular size. PCF-INH, in turn, presented a lower dissociation rate in the salt-rich aqueous medium, justifying its slower transport rate through the tissue. Taken together, these results suggest that INH-based metal complexes may be efficiently administered through the buccal route, impacting on both oral bioavailability and microbial resistance.

Formulation and Evaluation of Novel Hybridized Nanovesicles for Enhancing Buccal Delivery of Ciclopirox Olamine.

Ciclopirox olamine (CPO) is a topical wide-spectrum antimycotic agent that possesses antifungal, antibacterial and anti-inflammatory activities. Loading CPO into a hybridized vesicular system is expected to enhance its buccal permeation and hence, therapeutic activity, whereas the frequent administration and side effects are reduced. Vesicular systems with high penetration ability were prepared based on cholesterol, Lipoid S45 or Phospholipon 90H, with span 60 while incorporating a penetration enhancer (Labrafac or labrasol) followed by full assessment of their size, entrapment efficiency, and drug release profiles. The optimum formulation, composed of Lipoid S45 and Labrafac, possessed the smallest vesicle size (346.1nm), highest entrapment efficiency (94.4%), and sustained CPO release pattern, and was characterized for its morphology and thermal properties. This powerful mixture of the penetration enhancers (Lipoid S45 and Labrafac) in the designed hybridized vesicles was thoroughly investigated for their characteristics after being incorporated in bioadhesive gel. Moreover, enhanced antifungal activity was demonstrated either upon testing the designed formulation on agar plates or in vivo upon treating infected rabbits with the proposed formulation. Results suggest that the presented bioadhesive gel incorporating the CPO-loaded vesicles can be a promising delivery system that can offer a prolonged localized antifungal treatment with enhanced therapeutic effect.

Formulation and Physicochemical Characterization of Buccal Mucoadhesive Films Containing Alfuzocin Hydrochloride

The buccal region of oral cavity is a interesting target for the drug of choice administration. To increase prevent first pass metabolism and bioavailability, Alfuzocin Hydrochloride is embedded in buccal film for a sustained release over a period of 8 hours. The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive films of Alfuzocin hydrochloride using the polymers HPMC K100M, Sodium Alginate and Chitosan. The films were provided with a backing layer of Eudragit RS100 so as to get an unidirectional release pattern. The films were evaluated for their physical characteristics like weight, thickness, content uniformity, folding endurance, bioadhesive strength, surface pH, in vitro drug release, ex vivo buccal permeation and XRD studies. The films, which were prepared by the solvent casting method, were smooth and elegant in appearance; uniform in thickness, weight, and drug content; and showed good folding endurance. The mechanical properties reveal that the formulations were found to be strong but not brittle. The in vitro release data were fit to different equations and kinetic models viz. zero order, first order, higuchi’s plot and peppas plot. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation A7 (2% HPMC K100 M and 2% Chitosan). The correlation coefficient value (r) indicates, the kinetic of drug release was zero order. Stability study of optimized films was done and it was found that both drug and buccal films were stable. It can be concluded that the present buccal formulation can be an ideal system to improve the bioavailability of the drug by avoiding hepatic first-pass metabolism.

Formulation and Evaluation by Appling 32 (Three Squire) Factorial Design of Lercanidipine Hydrochloride Buccal Tablets with Mucoadhesive Polymers

Abstract: Aim: The aim of the present research work is to develop buccal tablets of Lercanidipine hydrochloride to reduce dosage frequency; obtain optimized and controlled therapy, better patient compliance. Materials and Methods: Lercanidipine HCL was obtained as a gift sample from Sun Pharma, Baroda, India. Other ingredients like Na-alginate, Carbopol 934 P, Micro Crystalline Cellulose, Mannitol, Magnesium stearate, Ethyl cellulose and Hydroxy Propyl Methyl CelluloseK4M were purchased from various sources. All other ingredients used were of analytical grade. Attempt was made by using mucoadhesive polymers HPMC K4 M, sodium alginate and carbopol 934 P in combination with Ethyl Cellulose as an impermeable backing layer. Results: Combination of polymer HPMC K4 M and sodium alginate release of drug was found in desired manner than other combinations. On the basis of the preliminary trials a 32 full factorial design was employed to study the effect of independent variables such as concentration of sodium alginate: HPMC K4M (X1) and type of filler (X2) on dependent variables. Factorial batches of F1 to F9 were formulated. HPMC K4M exhibited a much greater sustained effect on the release rate compared with sodium alginate. F4 shown the highest f2 value 70.46 and also all the h drug release was within the specified range. Based on the f2 value and targeted release profile the F4 batch was considered as optimized batch. Formulation F4 was subjected to an in vitro buccal permeation study. The results showed drug permeation of 99.04% in 12 h. The correlation between in vitro drug release rate and in vitro drug permeation across the chicken mucosa was found to be positive, with a correlation coefficient (R2) of 0.9921. Conclusion: From kinetic modelling of the dissolution profile of the optimized formulation, it was concluded that there is erosion-controlled release of Lercanidipine from the buccal adhesive drug delivery system. Key words: Lercanidipine hydrochloride, Buccal tablets, HPMC K4M, Buccal permeation study, Erosion controlled release.

Viscosity Effects of Hydrophilic Polymers on Transport of Collagen Hydrolysate Across Reconstructed Human Buccal Tissue

Herein we investigate the influence of hydrophilic polymers on the buccal permeability of collagen hydrolysate (CGH) by performing in vitro buccal permeation test and viscosity measurements. After we demonstrated that CGH (2000–3000 Da) could be delivered across the reconstructed human buccal tissue as evaluated by hydroxyproline assay, the effects of different hydrophilic polymers, varying amounts of CGH, and hydration methods were examined to elucidate the relationship with buccal permeation behavior of CGH. The percentage of CGH permeated was found to be highest in HPMC E5 solution and greater when the viscosity of test solutions was low. Using commercially obtained CGH‐loaded buccal films, the films under higher hydration condition exhibited greater CGH permeation. This study demonstrates that CGH can be delivered via the human buccal tissue and viscosity of the solution significantly affects the CGH permeation. These findings are valuable for designing hydrophilic polymer‐based buccal film formulations for peptides like CGH.