Drug Permeation Studies Research Articles

Design and Characterization of Atenolol Transdermal Therapeutic Systems: Enhancement of Permeability via Iontophoresis

The aim of the present investigation was to improve the permeation of Atenolol by preparing a transdermal patch and using the method of iontophoresis. Influence of chemical penetration enhancers was also studied. Combination of iontophoresis and chemical penetration enhancer d-limonene and oleic acid produced satisfactory permeation and flux. The electrically driven penetration enhancement provided by this method has succeeded in overcoming the formidable barrier presented by the stratum corneum, and has shown to be a promising technique for the transport of hydrophilic drug Atenolol from polymeric films. Atenolol is a water-soluble, ionizable drug and suffers from poor bioavailability when given by oral route due to its incomplete intestinal absorption and first-pass metabolism. Being a BCS class III drug, Atenolol has low log P (0.23) value, which also may be the reason for its poor intestinal absorption. Iontophoretic delivery using Ag/AgCl electrodes with current density of 0.35 mA/cm(2) enhances its delivery rate and thereby overcomes the problem of incomplete absorption. The prepared transdermal patches were subjected to ex vivo drug permeation studies using rat skin in phosphate buffer pH 7.4 for 24 h (passive and iontophoresis), and samples collected were analyzed by gradient high-pressure liquid chromatography. The column used was chiral alpha-glycoprotein (AGP) column (10 cm, particle size 5μ) and UV-detection at 225 nm was used. The effectiveness of permeation enhancers (d-Limonene and oleic acid) was determined by comparing drug flux in the presence and absence of each enhancer. Combination strategies of iontophoresis with chemical enhancers like oleic acid led to the significantly higher flux levels compared with passive transdermal delivery.

Localized delivery of cisplatin for the effective management of squamous cell carcinoma from protransfersome formulation

The present study is designed to investigate the local delivery of Cisplatin in cutaneous epithelial malignancies from protransfersome. Cisplatin-loaded protransfersome was prepared and characterized for size, zeta potential, surface morphology, percentage drug entrapment, in vitro drug permeation, vesicle-skin interaction, drug-excipients interaction, and stability study. An in vivo study was also performed to evaluate the efficacy of the proposed system. The size of the system was found to be 1115.56 ± 254 nm with zeta potential of -61.1 mV. Morphological studies revealed the defined structure of vesicles. The percentage entrapment of Cisplatin was found to be 97.97 ± 1.95% with skin permeation data of 560.20 ± 7.89 μg/cm(2). The presence of a fluorescence marker in the skin showed better skin penetration ability of the protransfersome. On comparison with IR spectra, it was clear that there was no significant interaction between the encapsulated drug and the excipients. In vivo performance of the system showed an increase in the therapeutic efficacy of drug with less systemic toxicity. The findings of the work appear to support improved, site-specific, and localized drug action, thus providing a better option to deal with skin-cited problems like squamous cell carcinoma. Further, the ultra-deformable nature of system seems to permit better delivery of the drug at the tumor site.

Preparation of Mucoadhesive Patches for Buccal Administration of Metoprolol Succinate: <i>In Vitro</i> and <i>In Vivo</i> Drug Release and Bioadhesion

Purpose: To develop mucoadhesive patches for buccal administration of metoprolol succinate and to evaluate their in vitro and in vivo bioadhesion.Methods: The mucoadhesive buccal patches were prepared by solvent casting technique using two different mucoadhesive polymers. The formulations were tested for in vitro drug permeation studies, buccal absorption, in vitro drug release studies, moisture absorption as well as for in vitro and in vivo bioadhesion.Results: The peak detachment force and work of adhesion for MC5 (sodium carboxymethylcellulose, i.e., Na CMC) patch were 0.87 N and 0.451 mJ respectively and the corresponding values for CH5 (chitosan) were 5.15N and 0.987 mJ. Formulation CH5 (prepared with chitosan) showed 67.1 % release, while MC5 (Na CMC) showed drug release of 81.9 % in 6 h. Basic pharmacokinetic parameters such as Cmax, Tmax and AUCtotal varied statistically (p < 0.05) when given by the buccal route compared with that of the solution given by the oral route.Conclusion: The results indicate that formulation of suitable bioadhesive buccal patches with the desired permeability is feasible. The development of bioadhesive buccal formulation for metoprolol succinate with a lower dose and few side effects may be attainable.Keywords: Mucoadhesive, Buccal patches, Metoprolol succinate, Sodium carboxymethylcellulose, Chitosan, Bioavailability

Novel application of Eudragit RL and cholesteryl oleyl carbonate to thermo-sensitive drug delivery system

The Eudragit RL 100 and propylene glycol (PG) membranes with and without cholesteryl oleyl carbonate (COC) were prepared by the solvent casting method to pioneer a novel application of a thermo-sensitive drug delivery system. After that, the properties of these membranes were investigated by thermal, scanning, and porosity studies. Drug permeation studies through all membranes were carried out using salbuthamol sulphate (SBS) at constant temperatures (25°C and 37°C), respectively. The permeability of SBS through the membranes with COC has been shown to be a discontinuous function of temperature, that is, their permeability increased steeply above the phase transition temperature (37°C) of the COC. The thermo-sensitive permeation mechanism for the membranes might be based on the structure change of the membranes caused by the phase transition, so that the membranes could absorb more water. Considering the high biological safety of Eudragit RL 100 and PG membranes with and without COC might be used to develop a novel thermo-sensitive drug delivery system.

Mesoporous Silica Nanoparticles for Increasing the Oral Bioavailability and Permeation of Poorly Water Soluble Drugs

We investigate the effects of spherical mesoporous silica nanoparticles (MSNs) as an oral drug delivery system to improve the oral bioavailability of the model drug telmisartan (TEL) and examine their cellular uptake and cytotoxicity. Further, we explore the mechanisms behind the improved oral absorption of poorly soluble drugs promoted by MSNs. An investigation of intestinal epithelial cellular binding, association and uptake was carried out by laser scanning confocal microscopy, transmission electron microscopy and fluorescence activated cell sorting. The results show that the cellular uptake is highly time-, concentration- and size-dependent. The model drug permeability studies in the human colon carcinoma (Caco-2) cell lines indicated that MSNs could significantly enhance TEL permeability and reduce rate of drug efflux. After loading TEL into MSNs, its oral bioavailability was compared with that of the marketed product Micardis and TEL-loaded ordered mesoporous silica microparticles (MSMs) in beagle dogs. The relative bioavailability of TEL-loaded MSN formulation and TEL-loaded MSM formulation was 154.4 ± 28.4% and 129.1 ± 15.6%, respectively. MSNs offer the potential to achieve enhanced oral bioavailability of poorly soluble drugs via improved drug dissolution rate and enhanced drug permeability.

Drug permeation studies of hydrogels usable for stimulus-induced local drug delivery systems

Drug permeation studies of hydrogels usable for stimulus-induced local drug delivery systems

Formulation and in Vitro, ex Vivo and in Vivo Evaluation of Elastic Liposomes for Transdermal Delivery of Ketorolac Tromethamine

The objective of the current study was to formulate ketorolac tromethamine-loaded elastic liposomes and evaluate their in vitro drug release and their ex vivo and in vivo transdermal delivery. Ketorolac tromethamine (KT), which is a potent analgesic, was formulated in elastic liposomes using Tween 80 as an edge activator. The elastic vesicles were prepared by film hydration after optimizing the sonication time and number of extrusions. The vesicles exhibited an entrapment efficiency of 73 ± 11%, vesicle size of 127.8 ± 3.4 nm and a zeta potential of −12 mV. In vitro drug release was analyzed from liposomes and an aqueous solution, using Franz diffusion cells and a cellophane dialysis membrane with molecular weight cut-off of 8000 Da. Ex vivo permeation of KT across pig ear skin was studied using a Franz diffusion cell, with phosphate buffer (pH 7.4) at 32 °C as receptor solution. An in vivo drug permeation study was conducted on healthy human volunteers using a tape-stripping technique. The in vitro results showed (i) a delayed release when KT was included in elastic liposomes, compared to an aqueous solution of the drug; (ii) a flux of 0.278 μg/cm2h and a lag time of about 10 h for ex vivo permeation studies, which may indicate that KT remains in the skin (with the possibility of exerting a local effect) before reaching the receptor medium; (iii) a good correlation between the total amount permeated, the penetration distance (both determined by tape stripping) and transepidermal water loss (TEWL) measured during the in vivo permeation studies. Elastic liposomes have the potential to transport the drug through the skin, keep their size and drug charge, and release the drug into deep skin layers. Therefore, elastic liposomes hold promise for the effective topical delivery of KT.

Formulation, optimization and evaluation of spray-dried mucoadhesive microspheres as intranasal carriers for Valsartan

This investigation deals with the intranasal delivery of Valsartan, encapsulated in HPMC-based spray-dried mucoadhesive microspheres, with an aim to provide rapid absorption and quick onset of action for treating hypertension. A 23-factorial design has been employed for the assessment of influence of three independent variables, namely inlet temperature, feed-flow rate and drug-polymer ratio on production yield, particle size and in vitro drug diffusion of the prepared microspheres. Microspheres were evaluated for particle size, entrapment efficiency, swelling property, in vitro mucoadhesion, in vitro drug diffusion, ex vivo drug permeation, histopathological examination and stability studies. The results of differential scanning calorimetry, X-ray diffraction and scanning electron microscopy revealed molecular dispersion of Valsartan into microspheres with spherical shape and smooth surface. Optimized formulation indicated good mucoadhesion with no severe sign of damage on nasal mucosa. Results of the non-invasive animal studies in dexamethasone-induced hypertensive rat model suggested the suitability of investigated drug delivery system for intranasal administration.

Application of simulated intestinal fluid on the phospholipid vesicle-based drug permeation assay

The compatibility of fasted state simulated intestinal fluid (FaSSIF) in drug permeation studies employing the phospholipid vesicle-based permeation assay (PVPA) model was confirmed by a set of different integrity indicators. Neither calcein permeability nor electrical resistance were found significantly changed indicating unaffected barrier tightness. Furthermore, the release of phospholipid from the barriers in contact with FaSSIF was negligible, although sodium taurocholate disappeared from the donor – possibly due to transfer into the barrier. Visual examination of the barrier structure by confocal laser scanning microscopy (CLSM) revealed no changes. The model drugs, cimetidine, nadolol, ketoprofen and griseofulvin showed either slightly enhanced or unchanged permeability values in the presence of FaSSIF. This may be attributed to micellar encapsulation and/or slight changes in barrier characteristics. Particularly for poorly soluble drugs, FaSSIF appeared favourable in terms of markedly improved recovery. Moreover, utilisation of BSA in the receiver compartment seems to augment this beneficial effect on recovery rate. It is likely that this experimental set-up affords better sink conditions in the receiver phase, which results in higher fluxes. Overall, a combination of FaSSIF in the donor phase and BSA in the receiver phase facilitates improved experimental output.

An investigation of the chick chorioallantoic membrane as an alternative model to various biological tissues for permeation studies

The chick chorioallantoic membrane (CAM) was explored as a biological membrane for use in the study of drug permeation with a Franz diffusion cell. The CAM was removed from fertilized chicken eggs of embryo age 9-18 days. The permeation profiles of nicotine through the fresh CAM were first obtained with a Franz diffusion cell. The permeation profiles of nicotine through frozen CAM, snake skin, pig skin, pig retina and pig buccal mucosa were also determined and compared with those of the fresh CAM. The permeability coefficient of the CAM varied with its age. The CAM at embryo age 13 was the most robust, showing the lowest standard error in permeability. It was thus chosen for comparative studies with snake skin, pig skin, retina and buccal mucosa. The CAM was found to be most similar to the buccal mucosa in terms of permeation profile and permeability coefficient values. Frozen CAM was also found to have a higher permeability coefficient than fresh CAM. The enhanced permeability was attributed to freezing, which affected the integrity of the CAM structure. From the findings, CAM shows potential as an alternative to the pig buccal mucosa as an in-vitro buccal model. The robustness of the CAM for drug permeation studies is affected by its age.

Formulation development and investigation of domperidone transdermal patches.

Aim and Background:Domperidone is a dopamine antagonist with antiemetic properties having a plasma half life of 7-9 h with 15% oral bioavailability. In the present work transdermal patches of domperidone were prepared with the objective to improve its therapeutic efficacy, patient compliance and to reduce the frequency of dosing and side effects, as well as to avoid its extensive first pass metabolism of the drug.Materials and Methods:The patches were prepared using ethyl cellulose (EC): Poly vinyl pyrrolidone (PVP), poly vinyl alcohol (PVA): Poly vinyl pyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC): Sodium (carboxy methyl cellulose) CMC as polymers in combination. The physicochemical parameters like thickness, drug content, weight variation, moisture absorption and drug permeation studies were evaluated for the prepared patches. No significant difference in thickness, average weight and in the drug content among the patches.Results:It was observed that from hydrophilic polymers the drug release was found to be faster compared to (F5 and F6 & F3 and F4) combination of hydrophilic and lipophilic polymers used in the study. Patches containing HPMC and Sodium CMC (F5 and F6) showed faster release as the patches showed maximum percentage amount moisture absorption. The in vitro release data was treated with kinetic equations and it followed Higuchi's diffusion mechanism. The in vivo bioavailability study was performed in rats and observed that, drug reached to the peak in approximately 60 min (16%) after oral route of administration. However, approximately same amount of drug was found in the serum from transdermal formulation in 6 h and further increase in the amount of drug in the serum, indicated that the drug 5 bioavailability could be better and hence the hepatic metabolism can be avoided, as it is evident from the data. Further, the decrease in the amount of drug present in the serum 45 min after oral administration also indicated that major amount of drug might have got metabolized and the bioavailability is reduced. However, the transdermal patch released further amount of drug (33%) at the end of 24 h.Conclusion:The present study can be concluded that transdermal patch can extend the release of drug for many hours with better bioavailability and also can avoid the first pass effect.

Design, Formulation and Evaluation of Transdermal Drug Delivery System of Budesonide

Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils, eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive first-pass metabolism in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4.. The major metabolites, 6-β- hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7: 2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation studies. These polymeric films were prepared by mercury substrate method employing PEG-400 as plasticizer. Two different penetration enhancers Urea and Dimethyl sulphoxide (DMSO) were employed in the study. The patches in each group were uniform in drug content, thickness. In Vitro drug permeation, moisture absorption and WVTR studies were carried out on these test patches. It was found that at all humidity condition the absorption increases which were linear to the moisture absorbed. In PVA and EUDRAGIT RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT condition the PVA and EUDRAGIT RL 100 patches provides the best resistance to water vapor. Therefore, when applied to animals (in further studies) these patches may provide more occlusion to water vapor loss from skin thus making atmosphere beneath the skin more humid that aid in drug permeation.

Preparation and in vitro characterization of the transdermal drug delivery system containing tamoxifen citrate for breast cancer

A matrix-type transdermal drug delivery system of tamoxifen citrate was developed by using a different ratio of eudragit- RL100, hydroxypropyl methyl cellulose (HPMC-K15), and ethyl cellulose (EC), by the solvent evaporation technique.The effect of the binary mixture of polymers with a penetration enhancer on the physical chemical parameters including, thickness, folding endurance, uniformity of drug content, moisture content, moisture uptake, tensile strength, and in vitro drug permeation were evaluated. The in vitro drug permeation studies were conducted by using modified Keshary-Chein diffusion cells through female Sprague Dawley rat skin using pH 7.4 phosphate buffer saline (PBS).The selected formulation’s stability studies were conducted as per the International Conference on Harmonization (ICH) guidelines, and did not show any degradation of the drug.

Formulation development and evaluation of in situ nasal gel of poorly water soluble drug using mixed solvency concept

The present study was aimed to develop a mucoadhesive in situ nasal gel containing domperidone with enhanced drug loading and transnasal permeation properties, which were achieved by improving drug solubility using the concept of mixed solvency. Poloxamer 407 was used as thermosensitive polymer and carbopol 934P as mucoadhesive polymer. Initially solubility of domperidone was enhanced in aqueous solution by using various solubilizers like sodium citrate (SC), urea (UR), polyvinyl pyrrolidone (PVP), polyethylene glycol (PEG), propylene glycol (PG) etc, individually and as a combination of two, three, and four solvents, respectively. Maximum solubility of domperidone was achieved at 30% w/w solvent concentration, containing mixed blend of PVP K30 (7.5% w/w) + PEG 400 (7.5% w/w) + PEG 600 (7.5% w/w) + Propylene Glycol (7.5% w/w), enhancing solubility of domperidone by 172.20 times as compared to its solubility in water. In situ gel was prepared by cold technique. Evaluation of the prepared gel was carried out, including properties like phase transition temperature, viscosity, in vitro drug release, drug content, transnasal permeation and stability studies. In vitro drug release studies of aqueous solution of mixed blend were performed and permeability coefficient was found to be 1.576 × 10-02 cm/hr and flux was found to be 8.64 μg/cm2hr. Similarly in vitro studies for in situ nasal gel were performed and percent cumulative drug release was 73.05±0.57% in 6 h.Transnasal drug permeation studies results in flux value of 7.04 μg/cm2hr and percent cumulative drug permeated across the membrane as 86.62±0.992%.The results from stability studies revealed that the prepared thermogel showed no significant decrease in drug content and no physicochemical change was observed upon storage in different temperature conditions resulting as a stable formulation.

Formulation design preparation and in vitro characterization of nebivolol transdermal patches

The aim of the present investigation is to develop and evaluate transdermal patches of nebivolol.The transdermal patches of nebivolol were prepared by solvent evaporation technique. Twelve formulations of nebivolol patches were prepared that composed of ethyl cellulose (EC) with hydroxyl propyl methyl cellulose (HPMC) and ethyl cellulose with polyvinyl pyrrolidine (PVP) in different ratios of 1:2, 1:4, 1:6, 2:1, 4:1, and 6:1 w/w, as film former. Polyvinyl alcohol (4% w/v) was used to prepare the backing membrane. All formulations contained Tween 80 (4% v/w) as penetration enhancer and propylene glycol (40% v/w) as plasticizer in dimethyl formamide as solvent system. The prepared transdermal patches of nebivolol were evaluated for thickness, mass variation, drug content, moisture content, moisture vapor transmission, folding endurance, tensile strength, ex vivo drug permeation study, drug release kinetics, scanning electron microscopy, primary skin irritancy study, and stability study. The physicochemical interactions between nebivolol and different polymers were studied by Fourier Transform Infrared (FTIR). The maximum drug release in 24 h was 95.185% (T2, HPMC:EC is 1:4), which is significant (P < 0.05). Furthermore, the formulation T2 showed maximum skin permeation (13.93 mg/cm2/h) in comparison with other formulations. The mechanical properties and tensile strength revealed that the formulations were found to be strong enough but not brittle. FTIR studies did not show any evidence of interaction between the drug and the polymers. Nebivolol matrix-type transdermal therapeutic systems could be prepared with the required flux having suitable mechanical properties.

Subtilisin-γ-Glutamyl Transpeptidase: A Novel Combination as Ungual Enhancer for Prospective Topical Application

A feather degrading strain of Bacillus licheniformis ER-15 was isolated which also degraded α-keratin of hooves. A detailed analysis revealed that a novel monomeric γ-glutamyl transpeptidase (GGT(30)), a proteolytic product of heterodimeric 67 kDa γ-glutamyl transpeptidase (GGT(67)), assists subtilisin during its action on α keratin. An equimolar combination of subtilisin and GGT(30) was designated as KerN and was used as ungual enhancer for topical application. KerN was effective in releasing proteins from nail plate surface and 300 µg of enzyme could release 41 µg protein/mg of nail after 24 h treatment. Scanning electron micrograph (SEM) revealed loosening of nail matrix confirming the action of KerN on nail keratin. Drug permeation studies revealed permeation of clotrimazole through both enzymatically pretreated nail plates and also through nail plates in presence of KerN. Nearly 58% drug could be retained by nail plates after 24 h of 300 µg/mL KerN which further enhanced up to 97% by prolonging the enzyme application. The enzyme was found to be stable in presence of drug even after 72 h. Thus, KerN can be used as an additive in formulation of topical drug for onchomycosis.

Magnetophoresis for enhancing transdermal drug delivery: Mechanistic studies and patch design

Magnetophoresis is a method of enhancement of drug permeation across the biological barriers by application of magnetic field. The present study investigated the mechanistic aspects of magnetophoretic transdermal drug delivery and also assessed the feasibility of designing a magnetophoretic transdermal patch system for the delivery of lidocaine. In vitro drug permeation studies were carried out across the porcine epidermis at different magnetic field strengths. The magnetophoretic drug permeation “flux enhancement factor” was found to increase with the applied magnetic field strength. The mechanistic studies revealed that the magnetic field applied in this study did not modulate permeability of the stratum corneum barrier. The predominant mechanism responsible for magnetically mediated drug permeation enhancement was found to be “magnetokinesis”. The octanol/water partition coefficient of drugs was also found to increase when exposed to the magnetic field. A reservoir type transdermal patch system with a magnetic backing was designed for in vivo studies. The dermal bioavailability (AUC 0–6 h ) from the magnetophoretic patch system in vivo, in rats was significantly higher than the similarly designed non-magnetic control patch.

Development and Characterization of Mucoadhesive In Situ Nasal Gel of Midazolam Prepared with Ficus carica Mucilage

The objective of the present study was to prepare mucoadhesive in situ nasal gels with mucilage isolated from fig fruits (Ficus carica, family: Moraceae) containing midazolam hydrochloride. Nasal gels of midazolam were prepared using three different concentrations (0.5%, 1.0% and 1.5% w/v) of F. carica mucilage (FCM) and synthetic polymers (hydroxypropylmethyl cellulose and Carbopol 934). Evaluation of FCM showed that it was as safe as the synthetic polymers for nasal administration. In situ gels were prepared with mixture Pluronic F127 and mucoadhesive agents. Evaluation of the prepared gels was carried out, including determination of viscosity, texture profile analysis and mucoadhesive strength. In vitro drug permeation study was conducted with the gels prepared with and without permeation enhancer (0.5% w/v sodium taurocholate) using excised goat nasal mucosa. In vitro permeation profiles were evaluated, and histological study of nasal mucosae before and after permeation study was also conducted to determine histological change, if any. In vivo experiments conducted in rabbits further confirmed that in situ nasal gels provided better bioavailability of midazolam than the gels prepared from synthetic mucoadhesive polymers. It was observed that the nasal gel containing 0.5% FCM and 0.5% sodium taurocholate exhibited appropriate rheological, mechanical and mucoadhesive properties and showed better drug release profiles. Moreover, this formulation produced no damage to the nasal mucosa that was used for the permeation study, and absolute bioavailability was also higher compared to gels prepared from synthetic polymers.

Fast Dissolving Sublingual Films of Ondansetron Hydrochloride: Effect of Additives on in vitro Drug Release and Mucosal Permeation

Ondansetron hydrochloride, a 5 HT3 antagonist is a powerful antiemetic drug which has oral bioavailability of 60% due to hepatic first pass metabolism and has a short half-life of 5 h. To overcome the above draw back, the present study was carried out to formulate and evaluate fast dissolving films of ondansetron hydrochloride for sublingual administration. The films were prepared from polymers such as polyvinylalcohol, polyvinyl pyrrolidone, Carbopol 934P in different ratios by solvent casting method. Propylene glycol or PEG 400 as plasticizers and mannitol or sodium saccharin as sweeteners were also included. The IR spectral studies showed no interaction between drug and polymer or with other additives. Satisfactory results were obtained when subjected to physico-chemical tests such as uniformity of weight, thickness, surface pH, folding endurance, uniformity of drug content, swelling index, bioadhesive strength, and tensile strength. Films were also subjected to in vitro drug release studies by using USP dissolution apparatus. Ex vivo drug permeation studies were carried out using porcine membrane model. In vitro release studies indicated 81–96% release within 7 min and 66–80% within 7 min during ex vivo studies. Drug permeation of 66–77% was observed through porcine mucosa within 40 min. Higher percentage of drug release was observed from films containing the sweeteners. The stability studies conducted for a period of 8 weeks showed no appreciable change in drug content, surface pH, and in vitro drug release.

Formulation and Evaluation of Buccal Patches for Delivery of Atenolol

Buccal patches for the delivery of atenolol using sodium alginate with various hydrophilic polymers like carbopol 934 P, sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose in various proportions and combinations were fabricated by solvent casting technique. Various physicomechanical parameters like weight variation, thickness, folding endurance, drug content, moisture content, moisture absorption, and various ex vivo mucoadhesion parameters like mucoadhesive strength, force of adhesion, and bond strength were evaluated. An in vitro drug release study was designed, and it was carried out using commercial semipermeable membrane. All these fabricated patches were sustained for 24 h and obeyed first-order release kinetics. Ex vivo drug permeation study was also performed using porcine buccal mucosa, and various drug permeation parameters like flux and lag time were determined.