Matrix Type Transdermal Patches Research Articles

Fabrication and Synthesis of Thiococlchicoside Loaded Matrix Type Transdermal Patch.

The goal of this work was to synthesize and fabricate matrix type transdermal patches based on a combination of polymers (Eudragit L100, HPMC and PVP K30), plasticizer and crosslinking agents (propylene glycol and triethyl citrate) and adhesives (Dura Tak 87-6908) to increase Thiocolchicoside (THC) absorption via topical route. This method allows avoidance of first-pass metabolism along with a consistent and extended duration of therapeutic activity. Fabrication and casting of polymeric solutions containing THC was done either in petri plates or through lab coater to get transdermal patches. Finally, the formulated patches were studied for their physicochemical and biological evaluation using scanning electron microscopy, FTIR, DSC, XRD and ex-vivo permeation studies using pig ear skin. FTIR studies confirm that the THC characteristics peaks (carbonyl (Amide I) at 1525.5 cm-1, C=O stretching (tropane ring) at 1664.4 cm-1, Amide II band (N-H stretching) at 3325.9 cm-1, thioether band at 2360.7 cm-1, and OH group stretching band at 3400.2 cm-1) are still present in the polymer mixture even after formulation as a transdermal patch, indicating compatibility among all excipients. While on the other hand, DSC studies confirm endothermic peaks for all the polymers along with THC with the highest enthalpy of 65.979 J/g, which is an indicator of sharp endothermic peak at 198°C, leading to the melting of THC. The percentage drug content and percentage moisture uptake of all the formulation was found in the range of 96 ± 2.04 to 98.56 ± 1.34% and 4.13 ± 1.16 to 8.23 ± 0.90%, respectively. Drug release and release kinetics studies confirm that it is dependent on the composition of individual formulation. All these findings support the possibility of using suitable polymeric composition, as well as proper formulation and manufacturing circumstances, to create a one-of-a-kind technology platform for transdermal drug administration.

Formulation and Evaluation of <i>Amomum sublatum</i> Leaf Oil Incorporated Pluronic Matrix Type Transdermal Patches in Percutaneous Absorption

A matrix type of transdermal patch formulations having different types of hydrophilic, hydrophobic polymer components Diclofenac potassium (Diclofenac K) served as the model drug and penetration enhancer for topical delivery in this research, employing the USP7 apparatus for dissolution studies. Transdermal patches loaded with Amomum sublatum leaf volatile oil (utilized penetration enhancer) were formulated using the solvent evaporation technique, incorporating varying amounts of pluronic F-127 and ethyl cellulose based on 15 formulations designed by the Box Behnken model. The prepared patches underwent evaluation for various physicochemical parameters, including tensile toughness, moisture content, and moisture uptake. In vitro diffusion studies were conducted using the USP7 apparatus dedicated to transdermal drug release investigations. The optimized formulation, F10, exhibited a drug release of 82% over 24 hours in the in vitro diffusion study. All the transdermal matrix-type formulations demonstrated satisfactory results, indicating that the developed matrix-type transdermal patch, containing different polymers and the A. sublatum leaf volatile oil penetration enhancer, holds potential for transdermal delivery in the treatment of pain and swelling.

Enhancing Transdermal Delivery: Investigating the Impact of Permeation Promoters on Ibuprofen Release and Penetration from Medical Patches-In Vitro Research.

This study investigated the impact of various enhancers on permeation through the skin and accumulation in the skin from acrylic pressure-sensitive adhesive-based drug-in-adhesives matrix-type transdermal patches. Eleven patches, each containing a 5% enhancer of permeation, encompassing compounds such as salicylic acid, menthol, urea, glycolic acid, allantoin, oleic acid, Tween 80, linolenic acid, camphor, N-dodecylcaprolactam, and glycerin, were developed. Ibuprofen (IBU) was the model active substance, a widely-used non-steroidal anti-inflammatory drug. The results were compared to patches without enhancers and commercial preparations. The study aimed to assess the effect of enhancers on IBU permeability. The adhesive properties of the patches were characterised, and active substance permeability was tested. The findings revealed that patches with 5% allantoin exhibited the highest IBU permeability, approximately 2.8 times greater than patches without enhancers after 24 h. These patches present a potential alternative to commercial preparations, highlighting the significant impact of enhancers on transdermal drug delivery efficiency.

Development and evaluation of matrix type transdermal patches of Simvastatin

Transdermal patches are a cutting-edge drug delivery technology, as it avoids first-pass metabolism results in increased bioavailability and aid in the delivery of drug molecules into the systemic circulation at predetermined and controlled rate. Aim behind this invention was to formulate a stable, reproducible and non-infringing & examine matrix-type transdermal patches of Simvastatin by using solvent evaporation method and the formulation consist various polymer including HPMC, Ethyl Cellulose, Chitosan, PVPK-30 and Eudragit RS 100, plasticizers like glycerine, propylene glycol, and trietholamine are utilised, along with solvents like octanol and ethanol. The prepared patches are assessed for thickness, weight variation, folding endurance, moisture content, drug content, surface pH and in vitro diffusion studies. The results indicated that the formulation P4 showed better characteristic properties and in vitro drug diffusion. Keywords: Transdermal drug delivery system, Simvastatin, HPMC, Eudragit RS100, Ethyl Cellulose.

Fabrication of solid lipid nanoparticles-based patches of paroxetine and their ex-vivo permeation behaviour

Paroxetine is not suitable for oral administration due to its extensive first-pass metabolism, thus resulting in less bioavailability. This study aimed to prepare novel paroxetine-loaded solid lipid nanoparticles (SLNs) based sustained-release transdermal patches to overcome these problems by enhancing drug absorption and bioavailability. Nine formulations of paroxetine SLNs were prepared by the hot melt-homogenization method using different concentrations of glycerol monostearate (Kolliwax) and Tween 80. Then these prepared SLNs were incorporated in a matrix type transdermal patch having a matrix of ethyl cellulose and polyvinyl pyrrolidone in 3:2 with polyvinyl alcohol. The SLNs showed a particle size range of 113–230 nm and an entrapment efficiency of 85.14%. The SLNs showed sustained paroxetine release (77.86–95.63% release) up to 48 h. FTIR studies showed no interaction between drug and formulation components. Paroxetine is evenly distributed in an amorphous form in SLNs, as demonstrated by DSC as well as PXRD analysis. SLNs formulated patches showed higher drug permeation through the skin than drug-based transdermal patches., Draize patch test revealed no sign of erythema after applying paroxetine-loaded SLN patches (score 0) as observed with the marketed product. The developed SLNs based transdermal patches showed increased permeability and sustained release behaviour.

Design and Evaluation of Solid Lipid Nanoparticle Loaded Transdermal Patch of Nisoldipine: In Vitro, Ex Vivo and In Vivo Evaluation

The objective of the research work is to develop and evaluate the solid lipid nanoparticles (SLNs) loaded matrix type transdermal patch of Nisoldipine (NSD). SLN formulations were developed and evaluated for particle size, zeta potential, polydispersibility index, drug content, entrapment efficiency then optimized formulation was freeze dried and incorporated into a transdermal patch. The physicochemical interaction between Nisoldipine and polymer was examined by DSC (differential scanning calorimetry) and FTIR (Fourier Transform Infrared Spectroscopy). Prepared patches were measured for thickness, uniformity of weight, folding endurance, moisture content, moisture absorption. The in-vitro and ex-vivo permeation of the Nisoldipine of the patches was studied by Franz diffusion cells. In vivo bioavailability study was performed using male wistar rats for optimized formulation N6 and compared with reference tablet (Sular). Dynasan 114 lipid (N-D4, formulation) is found to produce SLNs with low size and high entrapment efficiency. SEM analysis showed non aggregated spherical particles. N6(Formulation) patch containing 8% citral showed 96.5% of drug release and higher flux with 2.17 enhancement ratio (ER). Relative bioavailability of the test formulation with respect to market formulation was considered to be 2.52. The SLN loaded transdermal patches of Nisoldipine were developed successfully. There was considerable increase in bioavailability of the test formulation (N6) when compared to the marketed formulation. The increase may be attributed to avoidance of first pass metabolism of Nisoldipine which occurs through oral administration.

Development of matrix type transdermal Patches of Tizanidine HCl

Development of matrix type transdermal Patches of Tizanidine HCl

Fabrication and Evaluation of Controlled Release Transdermal Drug Delivery System of Carvedilol using Design Expert Software for the Management of Hypertension

Published on:August 2022Journal of Young Pharmacists, 2022; 14(3):295-301Original Article | doi:10.5530/jyp.2022.14.58 Authors: Saurabh Maan1, Roop Krishen Khar2, Rupa Mazumder3,*, Nishant Yadav1, Urooj Ahmed Khan4,* 1Department of Pharmaceutics, B.S. Anangpuria Institute of Pharmacy, Faridabad, Haryana, INDIA. 2Department of Pharmaceutics, B.S. Anangpuria Educational Institute, Faridabad, Haryana, INDIA. 3Department of Pharmacy, Noida Institute of Engineering and Technology, Greater Noida, Uttar Pradesh, INDIA. 4Department of Pharmaceutics, School of Medical and Allied Sciences, K.R Mangalam University, Sohna Road, Gurugram, Haryana, INDIA. Abstract: Objectives: Design, development and characterization of controlled release transdermal drug delivery system of carvedilol using Design Expert® software for managing hypertension. Materials and Methods: CV undergoes extensive first-pass metabolism due to low oral bioavailability approx ~24% and biological half-life ~6 hr. Available CV preparations have drawback of poor patient compliance due to increase in dosing frequency and making the therapy less effective. Phospholipid E80, glycerol and cholesterol were used for preparing CVGs via film hydration technique. Optimization was done using Central Composite Design under Design Expert software. While PVP and EC in a ratio of 4:1 in chloroform (5 mL) with plasticizer dibutyl phthalate (30%) were used for preparing Matrix type transdermal patch containing CVGs. Results: Optimized CVGs showed 115.7 nm particle size, and -16.4 mV zeta potential. TEM analysis also showed similar vesicle size and reveals globular structure of CVGs. Nearly 0.31 mm thickness, 0.14 % g weight variation, 99.13% flatness and 98.72% drug content was found in Matrix type transdermal patch having CVGs Transdermal patch with Franz diffusion cell showed approx. 90% release upto 48 hr during in-vitro permeation studies. In-vivo pharmacological assessment was done for efficacy estimation of GVs transdermal patch by N-nitro-L-arginine methyl ester which produced significant hypertension in rats. The application of CVGs transdermal patch resulted in a gradual decrease in BP, with the maximum effect from the patch observed at 10 hr (p < 0.001), the effect continued for 48 hr clearly indicating the gradual release of drug by transdermal patch for a long period. Conclusion: Developed novel transdermal patch having CV loaded glycerosomes may be considered as a promising approach for controlled release of drug with effective hypertension management. Keywords: Transdermal, Carvedilol, Design Expert, Glycerosomes, Hypertension, CCD.

Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch.

This study aimed to evaluate the effect of chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU] from the acrylic pressure-sensitive adhesive used as a drug-in-adhesives matrix type transdermal patch. The active substances tested were ibuprofen salts obtained by pairing the ibuprofen anion with organic cations, such as amino acid isopropyl esters. The structural modification of ibuprofen tested were Ibuprofen sodium salt, [GlyOiPr][IBU], [AlaOiPr][IBU], [ValOiPr][IBU], [SerOiPr][IBU], [ThrOiPr][IBU], [(AspOiPr)2][IBU], [LysOiPr][IBU], [LysOiPr][IBU]2, [PheOiPr][IBU], and [ProOiPr][IBU]. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also investigated. Thus, twelve transdermal patches with new drug modifications have been developed whose adhesive carrier is an acrylate copolymer. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. Our results show that the obtained ibuprofen patches demonstrate similar permeability to commercial patches compared to those with structural modifications of ibuprofen. However, these modified patches show an increased drug permeability of 2.3 to even 6.4 times greater than unmodified ibuprofen. Increasing the permeability of the active substance and properties such as adhesion, cohesion, and tack make the obtained patches an excellent alternative to commercial patches containing ibuprofen.

Cellulose Derivative-Based Bioadhesive Blend Patch for Transdermal Drug Delivery

In this study, matrix-type transdermal patches of glibenclamide were developed using a combination of hydrophilic and hydrophobic polymers for investigating the efficacy of transdermal carriers. A cellulose derivative, HPMC E50, was used as a hydrophilic matrix-forming polymer, and Eudragit RS 100 was used as a hydrophobic polymer. The solvent casting technique was employed to develop a transdermal blend patch formulation using chloroform and methanol as the casting solvent. No drug–polymer interaction was observed by the FTIR study. The membrane permeation study exhibited a sustained release of glibenclamide up to 12 h within a range of 76.15 ± 2.80% to 101.01 ± 0.33% depending on the polymeric ratio. The increased concentration of Eudragit RS 100 in different formulations has gradually decreased the amount of drug penetration through the membrane. The kinetic analysis showed the release is best explained by zero-order kinetics, followed by Higuchi and first order. The release exponent suggested shifting of non-Fickian diffusion to the super case II transport drug release mechanism when Eudragit RS 100 concentration was increased. It is concluded that the developed formulations may be a better alternative to the conventional oral delivery of glibenclamide.

Formulation and Evaluation of Hydrophilic Polymer Based Methotrexate Patches: In Vitro and In Vivo Characterization.

This study attempted to develop and evaluate controlled-release matrix-type transdermal patches with different ratios of hydrophilic polymers (sodium carboxymethylcellulose and hydroxypropyl methylcellulose) for the local delivery of methotrexate. Transdermal patches were formulated by employing a solvent casting technique using blends of sodium carboxymethylcellulose (CMC-Na) and hydroxypropylmethylcellulose (HPMC) polymers as rate-controlling agents. The F1 formulated patch served as the control formulation with a 1:1 polymer concentration. The F9 formulation served as our optimized formulation due to suitable physicochemical properties yielded through the combination of CMC-Na and HPMC (5:1). Drug excipient compatibilities (ATR-FTIR) were performed as a preformulation study. The ATR-FTIR study depicted great compatibility between the drug and the polymers. Physicochemical parameters, kinetic modeling, in vitro drug release, ex vivo drug permeation, skin drug retention, and in vivo studies were also carried out for the formulated patches. The formulated patches exhibited a clear, smooth, elastic nature with good weight uniformity, % moisture uptake, drug content, and thickness. Physicochemical characterization revealed folding endurance ranging from 62 ± 2.21 to 78 ± 1.54, tensile strength from 9.42 ± 0.52 to 12.32 ± 0.72, % swelling index from 37.16 ± 0.17 to 76.24 ± 1.37, and % drug content from 93.57 ± 5.34 to 98.19 ± 1.56. An increase in the concentration of the CMC-Na polymer (F9) resulted in increased drug release from the formulated transdermal patches. Similarly, drug permeation and retention were found to be higher in the F9 formulation compared to the other formulations (F1–F8). A drug retention analysis revealed that the F9 formulation exhibited 13.43% drug retention in the deep layers of the skin compared to other formulations (F1–F8). The stability study indicated that, during the study period of 60 days, no significant changes in the drug content and physical characteristics were found. ATR-FTIR analysis of rabbit skin samples treated with the formulated transdermal patches revealed that hydrophilic polymers mainly affect the skin proteins (ceramide and keratins). A pharmacokinetic profile revealed Cmax was 1.77.38 ng/mL, Tmax was 12 h, and t1/2 was 17.3 ± 2.21. In vivo studies showed that the skin drug retention of F9 was higher compared to the drug solution. These findings reinforce that methotrexate-based patches can possibly be used for the management of psoriasis. This study can reasonably conclude that methotrexate transdermal matrix-type patches with CMC-Na and HPMC polymers at different concentrations effectively sustain drug release with prime permeation profiles and better bioavailability. Therefore, these formulated patches can be employed for the potential management of topical diseases, such as psoriasis.

Detection and Analysis of Drug Crystals in Medical Transdermal Patches by Using X-ray Diffraction Measurement

The crystallization of active pharmaceutical ingredients (APIs) in matrix-type transdermal patches has implications for the rate of drug absorption through the skin and patch adhesion strength. Therefore, the presence or absence and the degree of API crystallinity must be controlled to guarantee the quality of patches. In this study, the utility of laboratory-level X-ray diffractometers for the detection and analysis of crystalline APIs in transdermal patches was investigated using medical patches of tulobuterol and isosorbide dinitrate. Several matrix-type patches employ a controlled drug delivery system containing intentionally crystallized API. Both benchtop and high-resolution laboratory X-ray diffractometers can detect several characteristic peaks of the APIs in these patches even if the patches are wrapped in an outer bag, although a benchtop model provides peak heights one-seventh to one-fifth that of a high-resolution instrument. An isosorbide dinitrate patch containing an unintentionally crystallized spot was wrapped in an outer bag, followed by measurements using both X-ray diffractometers. For both instruments, several isosorbide dinitrate-derived peaks were detected only at the crystallized spot, although the signal-to-noise ratio was poorer for the benchtop model. These results show that a high-resolution X-ray diffractometer is advantageous for high-detection sensitivity and offers a high degree of freedom of the measurement position on the sample. It was concluded that a laboratory-level high-resolution X-ray diffractometer can be used to examine the crystalline state of APIs in patches inside an unopened outer bag.

Development of monolithic matrix type transdermal patches containing cinnarizine: Physical characterization and permeation studies

Development of monolithic matrix type transdermal patches containing cinnarizine: Physical characterization and permeation studies

FORMULATION AND EVALUATION OF CLOPIDOGREL BISULFATE TRANSDERMAL PATCHES

Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. The main objective of the present work was to develop a suitable matrix type transdermal drug delivery system of Clopidogrel bisulphate using different polymers HPMC E15, Eudragit L100 and to compare the drug release through physical method and chemical method. Matrix type transdermal patches containing Clopidogrel Bisulfate were prepared by solvent evaporation technique. The prepared transdermal patches were evaluated for Thickness, folding endurance, tensile strength and in vitro studies. The prepared transdermal drug delivery system of Clopidogrel bisulphate using different polymers such as HPMC E15 and Eudragit L 100 had shown good promising results for all the evaluated parameters. Based on the In-vitro drug release, drug content and folding endurance results formulation F4 was concluded as an optimized formulation which shows its higher percentage of drug release.&#x0D; Keywords: Transdermal drug delivery, Clopidogrel bisulphate, HPMC E15, Eudragit L100

FORMULATION AND EVALUATION OF TRANSDERMAL PATCH OF PLUMBAGIN FOR ANTI-FUNGAL ACTIVITIES

The objective of the current study is to improve the patient compliance and sustained drug release action by herbal medicine which can be achieved by developing alternative drug delivery system. The matrix type transdermal patches containing plumbagin were prepared by solvent evaporation method with different ratios of polymers (HPMC 50cps, PVP K29-32 and EUDRAGIT RS-100). In these matrix type transdermal patches, the PEG (Polyethylene glycol) was used as plasticizer and DMSO (Dimethyl sulfoxide) used as a penetration enhancer. The formulated patches were evaluated for physicochemical parameters like thickness, weight variation, % moisture content, % moisture uptake, % flatness, folding endurance and drug content. In vitro drug release studies were carried out by using the Franz diffusion cell. The cumulative % of drug released in 10 hours from the six batch formulations were 95.66%, 94.2%, 97.33%, 90.13%, 83.75% and 85.71%, respectively. On the basis of in-vitro drug release, formulation (HE-2) was found to be better than other formulation and these were selected for further evaluation such as anti-fungal activity and stability studies.

Development and In Vitro Evaluation of Polymeric Responsive Release Matrix Type Transdermal Patches of Two Anti-asthmatic Drugs

Ketotifen fumarate, a mast cell stabilizer, and salbutamol sulfate, a bronchodilator, are frequently prescribed together for chronic asthma. This study aimed to combine both anti-asthmatic drugs in single polymeric responsive matrix type transdermal patches. Drug release from polymeric device was optimized by varying ratios of hydrophilic (polyvinyl pyrrolidone) and hydrophobic (ethyl cellulose) polymers. Propylene glycol was used as plasticizer and solvent system including mixture of chloroform and methanol. Physicochemical evaluations like thickness, weight variation, folding endurance, tensile strength, content uniformity and % moisture absorbance of developed patches were carried out. Developed patches were also subjected for in vitro release of drugs, and formulation of P6 with equal proportion of polyvinyl pyrrolidone and ethyl cellulose found optimized formulation with respect to release rate of both drugs. 76.49% of ketotifen fumarate and 77.49% of salbutamol sulfate were released from P6, and release of both drugs sustained up to 24 h. In the next step, permeability enhancers like Tween 20, isopropyl myristate, eucalyptus oil and span 20 were added to the formulation P6 and subjected to in vitro permeation study on Franz diffusion cell using rabbit skin. Results of in vitro permeation study revealed that transdermal patches with permeation enhancers permeate the significant amount of drugs in comparison with the formulation without enhancer.

Design and Development of Propranolol Hydrochloride Transdermal Patches: In Vitro and Ex Vivo Characterization

The main aim of this investigation is to design and develop matrix type transdermal patches of Propranolol Hydrochloride which is an anti-hypertensive drug. These matrix type transdermal patches were prepared by “Solvent Casting Technique” using drug, HPMC E15 and Eudragit L 100 in the ratio of 1:6, 1:6.5, 1:7, 1:7.5, 1:8, 1:8.5, 1:9, 1:9.5. All formulations carried 20%v/w of PEG-600 as plasticizer. The prepared patches were characterized for various physicochemical parameters like weight, thickness, folding endurance, drug content, percent moisture content, percent moisture absorption, in vitro drug release and ex vivo permeation. Among this 1:9 ratio was found to be an Optimized formulation and patches were prepared by using permeation enhancers (lemon grass oil, Eucalyptus oil, and clove oil). The cumulative amount of drug release in 12hrs for F7 formulation showed maximum and used for that formulation skin permeation on Goat abdominal skin. FTIR studies show no interaction between drug, polymer and other excipients. The drug permeation kinetics followed “First order” and “zero order” profile with diffusion mechanism.

Development and Evaluation of Matrix Type Transdermal Patches of Torasemide

TDDS manufacture has numerous benefits over other routes like oral delivery. It avoids limitations linked with g.i.t. absorption, enzyme effect, interaction with drug and food. This route is suitable when patient is suffering from vomiting and diarrhea. Torasemide is a loop diuretic; it comes under category of sulfonyl urea. It is prescribed in the treatment of edema, CHF, and hypertension. Whenever it is used by oral route, it is associated with many side effects like vomiting, nausea, anorexia, and increased appetite. All transdermal patches were transparent and free from any particle. Release profile of twelve batches of Torasemide was done by the means of Franz cell for 7 hrs. Maximum release was shown by MTP6 (71.28±0.19) and least in formulations of batch code MTP7(24.47±0.04). In-vitro release data were plotted in 2 different models i.e. first and Korsemeyer peppas. It was observed that release was governed by the diffusion process. On basis of different properties MTP1 batch was found to be optimum. Study concludes that by the means of patches Torasemide can be administered efficiently.&#x0D; Keywords: Torasemide, transdermal patches, HPMC, in-vitro release, stability studies, TDDS.

Nanoparticle formulations as recrystallization inhibitors in transdermal patches.

Drug crystallization in transdermal patches is still a major challenge, confronting the formulation development of topical drug delivery systems. Encapsulation of drugs into nanoparticles is proposed here as a promising tool for regulating drug crystallization in transdermal patches. The degree of recrystallization and transdermal permeation of ibuprofen and hydrocortisone loaded in polymeric and lipid nanoparticles from matrix-type transdermal patches were investigated. Ethyl cellulose (EC4), poly (lactide-co-glycolic acid) (PLGA) and polycaprolactone (PCL) were employed for polymeric nanoparticle preparations; while medium chain triglyceride (MCT) and witepsol were used for the preparation of MCT nanoemulsion and solid lipid nanoparticles (SLNs), respectively. As control, similar patches were prepared containing the free form of the investigated model drugs. All nanoparticle-containing transdermal patches exhibited less degree of drug recrystallization after 4weeks compared to the control groups. Among the investigated nanocarriers, transdermal patches formulated with drug-loaded lipid nanoparticles showed the lowermost degree of recrystallization. Drug encapsulation into SLNs succeeded to reduce the degree of ibuprofen and hydrocortisone recrystallization from 23.3±0.9 and 21.9±1.2% to 0.2±0.1 and 1.8±0.1%, respectively. Additionally, the decreased crystalline fraction was accompanied by a corresponding increase in the drug flux through excised pig skin, which was found to be correlated to the hydrophobicity of the different nanocarriers. In conclusion, polymeric and lipid nanoparticles proved to be effective tools for the preparation of transdermal patches with on-demand drug loadings, while lowering the recrystallization risks. Moreover, the results of this study can be a valuable guidance for the design of effective transdermal patches by controlling the crystallization of various drugs through fine tuning of the carrier hydrophobicity.

The Effect of Sodium Alginate, Hydroxy Propyl Methyl Cellulose E15 and Ethyl Cellulose N22 as Polymeric Matrices on the Physicochemical Characteristics of Meloxicam Patch

Meloxicam is an NSAID that can cause gastric irritation when orally administered. Transdermal drug delivery system can avoid its side effects and avoid first-pass metabolism in the liver. In this study, matrix type transdermal patches containing meloxicam were prepared using different ratios of sodium alginate, hydroxpropyl methylcellulose (HPMC) E15, and ethyl cellulose (3:2: 0.5; 2.5: 2:1; 2:2:1.5 and 1.5:2:2). The transdermal patches of meloxicam were prepared by mixing all dispersion polymers matrix and meloxicam. The patches were evaluated for physicochemical assessment (organoleptic, moisture content, surface morphology, drug content, and homogeneity). The result showed that there were differences in both moisture content and mass variation. The percent of moisture content and mass variation were increased as the amount of hydrophilic polymer increases. Formula 1.5:2:2 showed the best characteristic because it had low moisture content, however, it still needs further studies, such as stability, drug release, and penetration studies.