Transdermal Films Research Articles

DEVELOPMENT AND DESIGNING TRANDOLAPRIL TOPICAL FILM FOR MANAGEMENT OF CARDIAC STROKE

Transdermal drug delivery system (TDDs) is novel specified dosage forms, when drug deliver through the skin at controlled rate to the systemic circulation as applied to the intact skin. The present investigation is to prepared transdermal films of trandolapril intended for controlled release polymeric transdermal patch for a care of cardiac patients. The objective of current work is to develop the polymeric transdermal patch for immediate release of drug materials. The transdermal film of trandolapril was prepared by using various combinations of the polymers with solvent evaporation technique. The proposed formulations have a number of variables i.e. plasticizers, penetration enhancers, rate controlling process and adhesion on skin. We may apply biologically active permeation enhancers i.e. Isopropyl myristate, Propylene glycol and Mineral oils etc. The result concluded that polymers chitosan have hydrophilic nature and able to enhance spreadability and dispersibility of the water soluble trandolapril enhanced drug release more than 95.5% within a 6 - 7 h as needed for immediate release. The all evaluation parameters and in-vitro drug release study was used for selection of best polymeric film prepared with chitosan (2%) and PVP (1%) as plasticizer for the preparation of single layered transdermal film as first immediate release layer.

Formulation and Evaluation of Rosuvastatin Calcium Polymeric Nanoparticles-Loaded Transdermal Patch

Background: Transdermal drug delivery systems (TDDS) have been rapidly developed as a promising alternative to the oral delivery systems to provide controlled drug delivery and avoid the first-pass metabolism of drugs. Recently, various nanocarriers such as liposome and lipid nanoparticles have been used to enhance dermal and transdermal penetration of drugs. The aim of this study is to formulate and evaluate a polymeric nanoparticle (PNPs)-loaded transdermal patch of the antihyperlipidemic drug rosuvastatin. Materials and Methods: Rosuvastatin PNPs were prepared by nanoprecipitation method, and evaluated for particle size, zeta-potential and polydispersity index. PNPs-loaded patch and PNPs-free patch (control) of rosuvastatin were prepared by solvent casting method using hydroxyl polymethyl cellulose K15 (HPMC K 15) as film-forming polymer and polyethylene glycol 200 (PEG 200) as a plasticizer and evaluated for physical appearance, thickness, folding endurance, surface pH, in-vitro release and ex-vivo permeability. Results: The particle size, zeta-potential, and polydispersity index of rosuvastatin-loaded PNPs were 68.69 nm, - 7.5 mV, and 0.294, respectively. The prepared transdermal films showed acceptable appearance, thickness, and folding endurance as well as surface pH values. In vitro release study showed 65% and 82% cumulative release after 24 hrs for the polymeric nanoparticle-loaded patch and control patch, respectively. However. ex vivo permeation results showed that a significantly higher amount of rosuvastatin permeated via rat skin from the PNPs-loaded patch in comparison to the control patch (P-value ˂ 0.05). Conclusion: Rosuvastatin PNPs-loaded transdermal patch was successfully prepared and revealed promising releasing and permeation properties comparing to control patch.

An overview of preparation and characterization of solid binary system and its application on transdermal film with variation of plasticizers

Chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) is a problem, often occurs in patient. Inspite of high bioavailability, the demerits such as: hepatic first pass metabolism and invasive nature of oral and parenteral dosage forms can be avoided with anti-emetic therapy of transdermal device. The major objective of the present study is to modify the hydrochloride (HCl) form of Ondansetron (OND) to the base form followed by improvement of solubility and permeability of OND by employing solid dispersion (SD) loaded patches. Preformulation study, as observed, begins with an approach to enthuse solubility of OND by SD technique choosing different carriers. The choice of carriers was rationalized by phase solubility study. Several combinations of transdermal films were prepared with pure drug, carriers and SDs with plasticizer Ka values of OND-HPβCD binary system were found lower (54.43 to 187.57 M-1) than that of OND-PVP K-30 binary system (1156.77 to 12203.6 M-1). The drug content of SDs and patches were found satisfactory. Better permeation rate (236.48±3.66 µg/3.935 cm2) with promising flux enhancement (8.30 fold) was found with DBP loaded SD patch (P6*). Hence, enhancement of solubility and permeability of P6* ensures that it can successfully enhance the bioavailability.

Transdermal Film Loaded with Avanafil Ultra-deformable Nanovesicles to Enhance its Percutaneous Absorption and Bioavailability.

The in vitro dissolution of Avanafil (AVA) is the rate-limiting step for its bioavailability. Also, it undergoes the first-pass metabolism, and its absorption is altered significantly in the presence of food. So, our study aimed to overcome the previous hurdles and improve the AVA bioavailability by its incorporation in the ultra-deformable nanovesicles, transfersomes (TRF), then loading these nanovesicles in transdermal films. The AVA-loaded TRF formulation was optimized using Draper-Lin small composite design (D-LSCD). The optimized AVA-loaded TRF was evaluated for quality attributes and assessed for skin permeation using a fluorescence laser microscope and for pharmacokinetic parameters after topical application on the rats. The optimized AVA-loaded TRF showed a vesicle size of 97.75 nm, a zeta potential of -28.83 mV, and entrapment efficiency of 95.14% with good deformability and release profile. The intense discoloration in the deep skin layers of the rats indicated the permeation efficiency of AVA-loaded TRF films. The pharmacokinetic parameters specified the augmented absorption extent with Cmax of 254.66 ± 8.02 ng/mlversus 70.33 ± 3.05 ng/ml which reflected on the AUC0-inf that has a value of 2050.45 ± 159.14 ng/ml h versus 497.34 ± 102.61 ng/ml h for the optimized AVA-loaded TRF film and raw AVA-loaded film, respectively. These promising results wide open the field for broader clinical application of this alternative delivery pathway for superior bioavailability, efficacy, and patient compliance and satisfaction.

Cassava starch film loaded with extract of Piper betel leaf for anti-inflammatory activity

The aim of the present research work was to formulate a transdermal film of Piper betel L. leaf extract along with diclofenac sodium and evaluate its anti-inflammatory activity. The ethanolic extract of P. betel leaf was obtained by solvent extraction method using a Soxhlet apparatus. The P. betel leaf extract was analysed for inhibition of the albumin denaturation and it showed a significant inhibition of the albumin denaturation. The topical film was then prepared by solvent casting method using diclofenac sodium and P. betel leaf extract. The film was evaluated for drug content, thickness, weight uniformity, folding endurance, moisture content, moisture uptake, and barrier properties of the film. The formulated film was thin, flexible, and possessed satisfactory physicochemical properties. The anti-inflammatory potential of the film was evaluated by using carrageenan-induced rat paw oedema method on albino Wistar rats. The anti-inflammatory activity of film was found comparable with standard diclofenac sodium film and exhibited inhibition of oedema within 4 h. This signifies that the combination of P. betel leaf extract and diclofenac sodium has remarkable potential to serve as synergistic topical anti-inflammatory film preparation than simple topical film formulation of diclofenac sodium.

Oleic acid–reinforced PEGylated polymethacrylate transdermal film with enhanced antidyslipidemic activity and bioavailability of atorvastatin: A mechanistic ex-vivo/in-vivo analysis

To enhance the poor bioavailability and extensive liver metabolism of atorvastatin calcium (ATC), we have developed an oleic acid–reinforced PEGylated polymethacrylate (OLA–PEG–E-RLPO) transdermal film as a convenient and alternative delivery system. The effect of varying levels of Eudragit RLPO, PEG 400, and oleic acid on the target product profile was optimized through Quality by Design (QbD) approach. The ATC–loaded OLA–PEG–E-RLPO transdermal films were evaluated in ex-vivo experiments using full thickness skin, utilizing Franz cell studies, and undergone in-vivo pharmacokinetics/pharmacodynamics (PK/PD) assessment, using poloxamer-induced dyslipidemic Sprague-Dawley rats. At 2 and 12 h, the optimized ATC films with a thickness of 0.79 mm showed permeation of 37.34% and 97.23% into the receptor compartment, respectively. Steady-state flux was 0.172 mg/cm2h, with 7.01 × 10−4 cm/h permeability coefficient, and 0.713 × 10−3 cm2/h diffusion coefficient. In-vivo PK results indicated that the absorption profiles (AUC0-∞) of the optimized film in pre-treated group of animals were 8.6-fold and 2.8-fold greater than controls pre-treated with non-PEGylated non-oleic acid film and orally administered ATC, respectively. PD assessment of the lipid panel indicated that the lipid profile of the optimized film pre-treated group reached normal levels after 12 h, along with the significant enhancement over the non–PEGylated non-oleic acid film and the oral marketed tablet groups. The histopathological findings revealed near-normal hepatocyte structure for the optimized film pre-treated animal group. Our results further indicate that transdermal delivery films based on an optimized ATC–loaded OLA–PEG–E-RLPO were successfully developed and their assessment in both ex-vivo and in-vivo suggests enhanced permeability and improvement in bioavailability and antidyslipidemic activity of ATC. This approach can provide several advantages, especially during chronic administration of ATC, including improvement in patient compliance, therapeutic benefits, bioavailability, and feasibility for commercialization and as a platform for other drug classes.

Rethinking transdermal drug delivery using PVA-NLC based films

This work aims at designing an innovative poly(vinyl alcohol) (PVA) adhesive film containing nanostructured lipid carriers (NLC) loaded with olanzapine (OL) and simvastatin (SV), for the treatment of psychiatric disorders. Drug-in-NLC-in-PVA transdermal films were developed following a 32 full factorial planning. PVA concentration and lipid content were considered as key formulation variables. NLC formulations exhibited an average size of 177 ± 2 nm with a polydispersity index of 0.3 and a zeta potential of −20.8 ± 0.6 mV. The performance of PVA-NLC films was assessed in terms of adhesion, mechanical and transport (release and permeation) properties to obtain the best product conditions and providing a sustainable development process. Release kinetic studies showed that the PVA-NLC films enable a controlled drug release and that it depends on the concentration of PVA used. The formulation containing 12% (w/w) of PVA and 15% (w/w) of NLC provided the best permeation rate, along with adequate adhesiveness and cohesiveness, which is considered a promising therapeutic approach for further pre-clinical studies. An insight on the molecular details that govern the film construction and respective performance was provided by molecular dynamics simulations.

Investigating the Potential of Transdermal Delivery of Avanafil Using Vitamin E-TPGS Based Mixed Micelles Loaded Films.

To avoid the first-pass metabolism of avanafil (AVA) and its altered absorption in the presence of food after oral administration, this study aimed to investigate the potential of TPGS-based mixed micelle (MM)-loaded film for transdermal delivery and the enhancement of bioavailability. A Box–Behnken design was employed to optimize the permeation behavior of AVA from the transdermal film across the skin. The variables were the hydrophile-lipophile balance (HLB) of the surfactant (X1), the concentration of mixed micelles (MMs) in the film (X2), and the concentration of the permeation enhancer (X3). The initial permeation of AVA after 1 h (Y1), and the cumulative permeation of AVA after 24 h (Y2) were the dependent variables. Ex vivo studies were carried out on freshly isolated rat skin to investigate the drug’s permeation potential and results were visualized using a fluorescence laser microscope. Moreover, the pharmacokinetic behavior after a single application on male Wistar rats, in comparison with films loaded with raw AVA, was evaluated. The results showed that the optimum factor levels were 9.4% for the HLB of the surfactant used, and 5.12% MMs and 2.99% penetration enhancer in the film. Imaging with a fluorescence laser microscope indicated the ability of the optimized film to deliver the payload to deeper skin layers. Furthermore, optimized AVA-loaded TPGS-micelles film showed a significant increase (p < 0.05) in the Cmax of AVA and the area under the AVA plasma curve (approximately three-fold). The optimized AVA-loaded TPGS-MM film thus represents a successful delivery system for enhancing the bioavailability of AVA.

THYME OIL LOADED CASSAVA STARCH TRANSDERMAL FILM FOR WOUND HEALING

Biodegradable cassava starch-based transdermal film loaded with thyme volatile oil was prepared by solvent casting method for wound healing activity. The stretchability, water vapour permeability and antimicrobial properties of the film were measured. The films were evaluated for drug-excipient compatibility studies by Fourier transformed infrared spectroscopy (FTIR). The formulated film loaded with thyme volatile oil exhibited good anti-microbial activity against Staphylococcus aureus and Pseudomonas aeruginosa. The film was tested to determine its potential to increase the number of capillaries on the treated chick chorioallantoic membrane (CAM) surfaces using nine days old fertilized chick eggs. These thyme oil films loaded with cassava starch displayed angiogenic potential, which is required in the treatment of wound healing.

Transdermal Film Loaded with Garlic Oil-Acyclovir Nanoemulsion to Overcome Barriers for Its Use in Alleviating Cold Sore Conditions.

The exponentially mounting cases of herpes simplex virus infection or cold sores have become a serious global concern. Acyclovir (ACV) and garlic oil (GO)-loaded lipid nanocarrier could be a promising therapeutic approach in alleviating cold sores, as well as limiting the biopharmaceutical constraints associated with ACV absorption and therapeutic efficacy. Therefore, the objective of the current research study was to formulate an ACV-GO self-nanoemulsifying drug delivery system (ACV-GO-SNEDDS) as transdermal films. The prepared SNEDDS was optimized using an experimental mixture design. The optimized ACV-GO SNEDDS was loaded in transdermal film and was evaluated for ex vivo skin permeation and in vivo pharmacokinetic prospects. An optimized ACV-GO SNEDDs formulation constituted of 10.4% (w/w) of GO, 64.8% (w/w) of surfactant mixture (Tween 20®-Span 20®); 24.8%(w/w) of co-surfactant (Propylene glycol®), and 200mg of ACV, respectively, were prepared and characterized for particle size (Y). The observed globule size of the optimized ACV-GO SNEDDS is 170 ± 13.45 nm. The results of stability studies indicated that the stability index of optimized ACV-GO-SNEDDS was more than 92 ± 3%. This optimized ACV-GO SNEDDS was loaded in hydroxypropyl cellulose transdermal film. The outcome of the ex vivo skin permeation study demonstrated a 2.3-fold augmented permeation of ACV from the optimized ACV-GO SNEDDS HPC transdermal film in comparison to the raw ACV transdermal film. There was a 3-fold increase in the relative bioavailability of the optimized ACV-GO SNEDDS transdermal film compared to the raw ACV-HPC film. The study findings confirmed that the ACV-GO SNEDDS transdermal film exhibited excellent potential to enhance the bioavailability of ACV.

Formulation and Evaluation of Transdermal Film of Nitroglycerin

The aim of the present study was to prepare and evaluate transdermal Films of Nitroglycerin using HPMC, Cellulose acetate phthalate, ethyl cellulose and Polypropylene glycol as a rate controlling membranes and HPMC, Cellulose acetate phthalate, ethyl cellulose as drug reservoir gels. Transdermal Films of Nitroglycerin with HPMC, Cellulose acetate phthalate, ethyl cellulose by varying the blend ratios were prepared by solvent casting method. The thickness medium range between 0.18 ± 0.02 mm to 0.22 ± 0.03mm whatever signifies that they’re military uniform in thickness. The customized formulation NF1 acquires stability reports for one to three months and the general films were tested for drug content and In-vitro diffusion.

The Effect of Acid Modification of Porcine Mucin on Its Drug Release and Skin Permeation Properties in Insulin Transdermal Films

Background: The transdermal delivery of insulin involving the use of polymers has been extensively reported. More recently, the use of mucoadhesive or bioadhesive polymers as an insulin base in its formulation is gaining attention possibly due to the penetration enhancing properties of the polymers.&#x0D; Objectives: This study aimed at determining the effect of acid-modified porcine mucin powder on the release and permeation of insulin in transdermal films.&#x0D; Methods: Various batches of insulin films were prepared by solvent casting method using polysorbate 80 as an emulsifying agent and acid-treated and untreated mucin powders as a base. The films were evaluated for their physical properties, folding endurance, moisture content and uptake, drug content, bioadhesion, in vitro release, ex vivo permeation, and in vivo glucose-lowering activity.&#x0D; Results: The prepared insulin films had a weight range of 0.21-0.27 g, folding endurance of 101-103, moisture content and uptake of 13.73%-18.57% and 11.70%-22.30%, respectively, and drug content of 96%-101%. The bioadhesion of the films prepared with acid-treated mucin was within the range of 0.088-0.186 Nm-1 as against 0.055 Nm-1 of the films prepared with untreated mucin. The in vitro release profiles showed a release of 95% insulin from films prepared with untreated mucin within 2 h while the films made with acid-treated mucin gave a release of about 60%-73% over the same period, indicating a slower release. Animals that received acid-treated mucin-base insulin films showed delayed but sustained blood-glucose-lowering up to 70% and for films prepared with untreated mucin 55% within 12 h. &#x0D; Conclusion: Insulin transdermal films prepared with acid-modified mucin powder gave superior bioadhesive strength values. They also showed improved drug permeation enhancing ability and achieving up to 70% blood glucose lowering in diabetic rats.

Design and optimization of process parameters of polyvinyl alcohol-graft-lactic acid films for transdermal drug delivery

The objective was to apply a simplex lattice design to determine the properties of polyvinyl alcohol-graft-lactic acid (PVA-g-LA) with different values for two independent variables: curing time (X1) and LA ratio (X2). Each independent variable was varied among three levels: -1, 0, and +1. Three coded levels were 120 min, 150 min, and 180 min for X1 and 2.5 g, 5 g, and 7.5 g for X2. Dependent variables of swelling behavior in various swelling media and thermal analysis parameters were monitored. The optimal formulation was selected based on the desirability value. The prediction was accurate, showing a low value of percent error. The morphology of the selected formulation with the highest desirability value showed a compact and dense film. Propranolol hydrochloride used as a model drug, was loaded into PVA-g-LA film. The propranolol hydrochloride content was 4.19 ± 1.05 mg/cm2. The cumulative release and permeation of drug were 61.94 ± 8.03% and 59.96 ± 6.61%, respectively. Thus, response surface methodology can be used as a tool to predict or optimize the process parameters for PVA-g-LA transdermal films in an accurate manner. PVA-g-LA could control the release and permeation of drug from the film layer.

An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device

Chemotherapy induced nausea and vomiting (CINV) is an issue, which usually occurs in cancer patient. Despite high bioavailability of oral and intravenous administration, these have some drawbacks. The oral route causes hepatic first pass metabolism and intravenous route is invasive in nature. Hence, antiemetic drug by means of transdermal route is necessary to administer in such cases. The aim of the present investigation is to develop suitable Transdermal Therapeutic System (TTS) with an objective to enhance solubility and skin permeability properties of metoclopramide base. Preformulation study begins with an approach to enhance solubility of 40 metoclopramide base by solid dispersion technique. transdermal films were prepared with 41 the solid dispersion as well as with pure drug. Phase solubility study at various temperatures reveals binding constants (Ka, 95-350 M-1 for PVP K30; 56-81 M-1 for HPβCD). Spontaneity of solubilization was justified by AL type linear profiles. The films showed satisfactory diffusion (%), permeation rate and flux after 8 h study. The transdermal patches as prepared were analyzed under FTIR, DSC and SEM. Both solubility and permeability rate in this investigation have been enhanced. So, it can be affirmed that this route would effectively enhance bioavailability

Rifampicin-Loaded Alginate-Gelatin Fibers Incorporated within Transdermal Films as a Fiber-in-Film System for Wound Healing Applications.

The various biological and molecular cascades including different stages or phases such as inflammation, tissue proliferation, and remodeling phases, which significantly define the wound healing process. The natural matrix system is suggested to increase and sustain these cascades. Biocompatible biopolymers, sodium alginate and gelatin, and a drug (Rifampicin) were used for the preparation of fibers into a physical crosslinking solution using extrusion-gelation. The formed fibers were then loaded in transdermal films for wound healing applications. Rifampicin, an antibiotic, antibacterial agent was incorporated into fibers and afterwards the fibers were loaded into transdermal films. Initially, rifampicin fibers were developed using biopolymers including alginate and gelatin, and were further loaded into polymeric matrix which led to the formation of transdermal films. The transdermal films were coded as TF1, TF2, TF3 and TF4.The characterization technique, FTIR, was used to describe molecular transitions within fibers, transdermal films, and was further corroborated using SEM and XRD. In mechanical properties, the parameters, such as tensile strength and elongation-at-break (extensibility), were found to be ranged between 2.32 ± 0.45 N/mm2 to 14.32 ± 0.98 N/mm2 and 15.2% ± 0.98% to 30.54% ± 1.08%. The morphological analysis firmed the development of fibers and fiber-loaded transdermal films. Additionally, physical evaluation such as water uptake study, water transmission rate, swelling index, moisture content, and moisture uptake study were executed to describe comparative interpretation of the formulations developed. In vivo studies were executed using a full thickness cutaneous wound healing model, the transdermal films developed showed higher degree of contraction, i.e., 98.85% ± 4.04% as compared to marketed formulation (Povidone). The fiber-in-film is a promising delivery system for loading therapeutic agents for effective wound care management.

Investigation of Polymeric Micellar Nanoparticles of Amlodipine Besylatefor Transdermal Delivery

: Objectives: The objective of this study was to formulate and investigate amlodipine besylate loaded polymeric micelles and their effect on enhancing transdermal permeation of the poorly water-soluble drug via transdermal films. Methods: Pluronic F127 and Pluronic F68 polymers were chosen to prepare micelles in different drug – polymer ratios. Prepared formulations were characterised for surface morphology, micelle size, polydispersity index, zeta potential, loading efficiency, percentage drug weight in micelles and stability. Optimized amlodipine micelle dispersions were incorporated into hydroxypropyl methylcellulose K100 and polyvinyl pyrrolidone K30 transdermal films prepared by the solvent casting method. These films were evaluated for thickness, percentage weight variation, folding endurance, moisture absorbance, percentage drug content, ex vivo permeation and in vivo skin irritation. Results: Selected micelle formulations had the desired vesicle size, homogeneity and stability. Scanning electron microscopy show spherical vesicles. Micelle incorporated transdermal films were smooth, flexible, translucent and mechanically strong. The ex vivo skin permeation studies reveal that the flux of amlodipine besylate from the micelle incorporated transdermal films was significantly higher than that containing the free drug, confirming the drug solubilizing effects of micelles. Reconstitution of micelles from optimized films revealed that the original characteristics of the micelles were intact. Studies in Wistar rats showed that the prepared transdermal films were free of irritation potential when evaluated by the Draize dermal irritation scoring system. Conclusion: Beside their solubilizing effect, Pluronic micelles could be useful as novel drug carriers for enhancing transdermal permeation of Amlodipine besylate and thus its bioavailability.Key words: Hydroxypropyl methylcellulose, Micelle, Nanoparticle, Permeation, Pluronic, Skin irritation.

Formulation optimization and characterization of transdermal film of curcumin by response surface methodology

ObjectiveIndia is referred as goldmine of herbal drugs but still lack of optimization of herbal drugs, which has kept us on the back foot. The rationale of the study is to prepare optimized transdermal drug delivery system of curcumin employing response surface methodology to study the collective effect of independent variables like concentration of ethyl cellulose, hydroxyl propyl methyl cellulose and dibutyl phthalate which significantly influenced characteristics like percentage elongation and in vitro drug release. MethodTwenty formulations containing varying concentrations of polymers and permeation enhancer were prepared using solvent casting technique. ResultThe study revealed that the effect of dibutyl phthalate (DBP) concentration was the highest on percentage elongation (P < 0.0001), while hydroxy propyl methyl cellulose (HPMC) concentration exhibited pronounced effect on drug release (P < 0.0001) through dialysis membrane. Linear model fitted the best for curcumin release and elongation for all formulations. According to Derringer’s desirability prediction tool, the composition of optimized film was found to be 242.14% of HPMC, 109.59% of ethyl cellulose (EC), and 1.03% of DBP. Under these conditions, the optimized patch exhibited a predicted value of %elongation and in vitro drug release of 94.35% and 80.0306%, respectively, which was comparable to the actual values of percent elongation and in vitro drug release i.e. 95.02% and 81.03% respectively. FTIR and thermal studies were also performed which revealed no interaction or complexation between drug and excipients. The ex vivo study performed using rat skin showed that the cumulative drug release from the optimized patch showed flux of (30.68 ± 18) µg/cm2/h. ConclusionIt can be concluded that in future if proper optimization of herbal formulations is carried out, they can become the first choice for patients as compare to synthetic drugs.

Evaluation of Transdermal Formulations of Metoclopramide Prepared Using Arachis Oil and Liquid Paraffin as Permeation Enhancers

Background: The study aimed to evaluate the effect of arachis oil and liquid paraffin on metoclopramide release from transdermal films.&#x0D; Objectives: Batches of metoclopramide films were prepared with hydroxypropyl methyl cellulose (HPMC), arachis oil or liquid paraffin and Tween 80 as plasticizer. The films were evaluated for their physiochemical properties, in vitro and ex vivo drug release and drug release kinetics. Drug-excipient interactions were investigated using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy.&#x0D; Methods: The transdermal films had a weight range of 0.22-0.24 g, folding endurance of 300-306, percentage moisture content and uptake of 2%-10% and 19%-110%, respectively and drug content of 98%-104%. There was similar condition in vitro release profile for the films but their ex vivo profiles exhibited variable drug release with the P3 (30% arachis oil) giving the highest drug (almost 100%) release. &#x0D; Results: The release kinetics of metoclopramide followed the first order and Korsemeyer-Peppas models more closely as seen in their correlation coefficients (R2) of 0.9832 and 0.9560, respectively. Drug-excipient compatibility studies showed no interactions between excipients and metoclopramide.&#x0D; Conclusion: The formulated transdermal films showed controlled drug release over a period of 12 h. Arachis oil and liquid paraffin showed similar permeation enhancing ability. These enhanced permeation properties of the films could be helpful in the development of alternative route for metoclopramide administration in the management of emesis with improved patient acceptance.

Effect of Plasticizer on Delivery of Valsartan from Tamarind Gel Based Transdermal Film Formulation

Effect of Plasticizer on Delivery of Valsartan from Tamarind Gel Based Transdermal Film Formulation

Preparation and Characterization of Ivabradine HCl Transfersomes for Enhanced Transdermal Delivery

Ivabradine HCl (IVB) is used in treatment of stable angina pectoris. The aim of the work was to prepare a once daily transdermal film of transfersomes loaded IVB. Transfersomes were prepared by modified ethanol injection method using three formulation factors namely: surfactant type, drug: phospholipid ratio and surfactant: phospholipid ratio. The transfersomes were characterized for entrapment efficiency, particle size, zeta potential, in vitro drug release, optical and transmission electron microscopy imaging, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The best transfersomes showed optimal properties as well as pure drug were further formulated in transdermal film and characterized for content uniformity, folding endurance, weight and thickness, moisture content, moisture uptake, tensile strength and permeation through excised ear rabbit skin. Pharmacokinetic parameters of transfersomes incorporated film were compared with oral solution of the same drug dose. A maximum of about 82.03% entrapment efficiency, size of 206.7 nm, zeta potential of −88.3 Mv and 66.7% of drug release after 24 h were obtained from sodium lauryl sulphate based transfersomes at drug: phospholipid and surfactant: phospholipid ratio of 1:20 and 75:25 w/w, respectively. Films contained IVB transfersomes exhibited improved permeability and skin retention when compared with pure drug as well as enhanced pharmacokinetic parameters.