scholarly journals Application of Factorial Design for Optimization of PVC-HPMC Polymers in Matrix Film Ibuprofen Patch-Transdermal Drug Delivery System

2020 ◽  
pp. 11
Author(s):  
Galih Pratiwi ◽  
Susi Susanti ◽  
Shaum Shiyan
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Transdermal Drug Delivery System ◽  
Control Drug ◽  
Matrix Optimization ◽  
The Matrix ◽  
Optimum Formula

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) class of drugs, and oral use can cause side effects. Transdermal patch dosage forms are useful for minimizing side effects on oral administration. Transdermal patches are formulated using a special membrane that can control drug release in the matrix system. This study was intended to determine the characteristics of the resulting patch, the optimum composition of the formula, and the profile of the release of transdermal ibuprofen release. The film matrix optimization on the ibuprofen patch formulation uses design of experiment (DoE) approach using factorial design 22. The mixture of polyvinyl pyrrolidone (PVC) and hydroxypropyl methylcellulose (HPMC) components gives a pleasant texture, and the release results in vitro show a proper and controlled release of the ibuprofen patch. Based on the research, it can be concluded that the patch has excellent characteristics with a good texture so that the development time is long with the optimum formula of chitosan and HPMC, as well as having a proper and controlled release profile.

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

scholarly journals EFFECT OF POLYMERS ON THE PHYSICOCHEMICAL AND DRUG RELEASE PROPERTIES OF TRANSDERMAL PATCHES OF ATENOLOL

2018 ◽  
Vol 10 (4) ◽  
pp. 68
Author(s):  
Manish Kumar ◽  
Vishal Trivedi ◽  
Ajay Kumar Shukla ◽  
Suresh Kumar Dev
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
High Moisture ◽  
Transdermal Drug Delivery System ◽  
Permeable Membrane ◽  
Transdermal Patches ◽  
Egg Membrane ◽  
Hydrophilicity And Hydrophobicity

Objective: The objective of this research work was to develop a transdermal drug delivery system containing atenolol with different ratios of hydrophilic and hydrophobic polymeric combinations, using solvent evaporation technique and to examine the effect of hydrophilicity and hydrophobicity of polymers on the physicochemical and drug release properties of transdermal patches.Methods: Solvent casting method has been used to formulate transdermal patches. Hydroxypropyl methylcellulose (HPMC), Polyvinylpyrrolidone (PVP), Ethylcellulose (EC) in different combination ratios were used as the polymer. Propylene glycol was used as a plasticizer. Permeation enhancers such as span 80 were used to enhance permeation through the skin. In vitro diffusion study was carried out by franz diffusion cell using egg membrane as a semi-permeable membrane for diffusion.Results: Result showed that the thickness of the all batch of patches varied from 0.32 to 0.39 mm with uniformity of thickness in each formulation. Formulations F1 to F3 had high moisture content varied from 2.07±0.09 to 2.56±0.15 and high moisture uptake value varied from 3.21±0.35 to 4.09±0.38, due to a higher concentration of hydrophilic polymers. Drug content of all batches was ranged between 85.92±1.32 to 95.71±1.42. Folding endurance values off all batches were more than 75. Formulation batches F1 to F3 showed higher cumulative drug release varied from 61.34% to 68.11% as compared to formulation batches F4 to F6.Conclusion: Higher proportion of hydrophilic polymer in the formulation of transdermal patches, gives higher percentage drug release from prepared patches. The finding of the study indicates that hydrophilicity and hydrophobicity of polymer effects the physicochemical and drug release properties of transdermal patches and an optimum proportion of hydrophilic and hydrophobic polymer is required for the preparation of effective transdermal patches. 

scholarly journals FORMULATION AND EVALUATION OF PROCHLORPERAZINE MALEATE SUSTAINED RELEASE FLOATING TABLET

2017 ◽  
Vol 9 (2) ◽  
pp. 89 ◽  
Author(s):  
Ahmed Abdulameer Albadry ◽  
Wedad K. Ali ◽  
Fouad A. Al-saady
Keyword(s):  
Chemical Interaction ◽  
Hydroxypropyl Methylcellulose ◽  
Angle Of Repose ◽  
Weight Variation ◽  
Compressibility Index ◽  
Floating Drug Delivery ◽  
Tap Density ◽  
Floating Tablet ◽  
Optimum Formula

<p><strong>Objective: </strong>The objective of this study was to formulate once daily sustained oral release floating tablet of prochlorperazine maleate, this floating tablet has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility.</p><p><strong>Methods: </strong>The prochlorperazine maleate floating tablets were formulated by using hydrophilic swellable polymer and gas generating agent. In this study, 15 formulas were prepared with many variables in order to achieve an optimum dissolution and floating behaviour for the floating tablet. The all prepared formulas were tested for bulk density, tap density, angle of repose, Carr's Index, thickness, weight variation, hardness, friability, drug content, <em>in vitro</em> dissolution test, <em>in vitro </em>buoyancy, and swelling index.</p><p class="Default"><strong>Results: </strong>Formula (F2) that contain 55% (w/w) <a href="https://www.google.iq/url?sa=t&amp;rct=j&amp;q=&amp;esrc=s&amp;source=web&amp;cd=3&amp;ved=0ahUKEwjh383ow9LPAhWF6RQKHRChCVgQFggpMAI&amp;url=https%3A%2F%2Fwww.ulprospector.com%2Fen%2Fna%2FFood%2FDetail%2F895%2F563462%2FBenecel-Hydroxypropylmethylcellulose-HPMC-K4M&amp;usg=AFQjCNGgfyJECkumK5cpU_6luVwwJ2fKxA&amp;bvm=bv.135258522,d.d24">hydroxypropyl methylcellulose</a> k4M (HPMCK4M), 5 % (w/w) sodium bicarbonate (NaHCO<sub>3</sub>) have acceptable flow properties and compressibility index and good physical properties with floating lag time (16±0.57) seconds and total floating time (32±0.29) h with 100% release of prochlorperazine maleate at the end of 24 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F2) showed no chemical interaction between the drug and the excipients that used in the formula.<strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that that the selected formula (F2) can be a promising formula for the preparation of gastro retentive floating drug delivery systems of prochlorperazine maleate.</p>

scholarly journals Development and evaluation of miconazole mucoadhesive tablets for oropharyngeal candidiasis

2017 ◽  
Vol 16 (10) ◽  
pp. 2325-2330
Author(s):  
Qiong Jin ◽  
Wei Chen ◽  
Wan Wu
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Extended Period ◽  
Content Uniformity ◽  
Oropharyngeal Candidiasis ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Mucoadhesive Tablets

Purpose: To develop mucoadhesive tablets containing miconazole (MCZ) for the treatment of oropharyngeal candidiasis, using chitosan and hydroxypropyl methylcellulose (HPMC) as mucoadhesive polymers.Methods: Mucoadhesive tablets were formulated and optimized using a 23 factorial design and direct compression method. The independent variables were compression force and concentrations of chitosan and HPMC, while mucoadhesion time and in vitro drug release were dependent variables. Tablet characterization was carried out by evaluating hardness, thickness, tablet weight variation, content uniformity, friability and in vitro drug release at salivary pH (pH 6.8).Results: The tablets showed good mucoadhesion for an extended period (8 h), and their physical characteristics were within acceptable ranges. Drug release ranged from 60.5 % to 80.8 %.Conclusion: These results indicate that the mucoadhesive MCZ tablets formulated with chitosan and HPMC possess potential for the development of therapeutic preparations for management of oropharyngeal candidiasis.Keywords: Miconazole, Oropharyngeal candidiasis, Factorial design, Mucoadhesion, Chitosan, Drug release

scholarly journals DESIGN, FORMULATION, AND CHARACTERIZATION OF APREMILAST-SACCHARIN COCRYSTALS LOADED WITH TOPICAL GEL

2020 ◽  
pp. 60-67
Author(s):  
TEJASWINI MANE ◽  
MUKESH MOHITE
Keyword(s):  
Physicochemical Properties ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Gelling Agent ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Topical Gel ◽  
Solubility Study

Objective: Most of the drugs are relevant to BSC class II and class IV having solubility problems. Cocrystallization of drug with conformer is an immense approach used to explore the physicochemical properties of drug. The objective of the present work was to design formulate and evaluate the drug cocrystals of poorly soluble drug apremilast (APR) with saccharin. Methods: Cocrystals of APR were prepared using the solvent evaporation technique. The saturated solubility study and in vitro dissolution study of cocrystals were carried out. The prepared cocrystals were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy. The topical gel of APR cocrystals was formulated optimized and evaluated using three-level factorial design. Results: The cocrystals of APR were prepared in 1:1 molar ratio with saccharin. APR cocrystals showed the improvement in solubility and dissolution as compared to pure APR. The formation of cocrystals was confirmed from change in endothermic peak of DSC and from shifting of FTIR spectra of cocrystals. Crystallinity of cocrystal was confirmed from XRD pattern and noteworthy change in 2θ values of the intense peak. The topical gel of APR cocrystals was formulated and optimized using three-level factorial design using Carbapol-940 and hydroxypropyl methylcellulose (HPMC) as a gelling agent. Conclusion: The cocrystals with altered physicochemical properties of APR were prepared with saccharin and formulated as a topical gel to overcome the problems related to oral administration.

scholarly journals Preparation and evaluation of an ispaghula based directly compressible matrixing agent for controlled release

2008 ◽  
Vol 58 (3) ◽  
pp. 309-316 ◽  
Author(s):  
Anita Lalwani ◽  
Jolly Parikh
Keyword(s):  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Hydrogen Phosphate ◽  
Lattice Design ◽  
Phosphate Dihydrate ◽  
Simplex Lattice Design ◽  
Dependent Variables ◽  
Simplex Lattice ◽  
Preparation And Evaluation

Preparation and evaluation of an ispaghula based directly compressible matrixing agent for controlled releaseThe objective of the present investigation was to prepare and evaluate an ispaghula husk based directly compressible (DC) adjuvant that can be used as matrixing agent using an agglomeration technique. Addition of hydroxypropyl methylcellulose was found necessary to improve cohesion. Lactose (X1), calcium hydrogen phosphate dihydrate (X2) and Avicel PH101 (X3), used along with ispaghula in preparation of agglomerates, were selected as three independent variables in a simplex lattice design affecting compressional and dissolution characteristics of the drug from the DC adjuvant. The agglomerates were evaluated for their flow properties. Tablets were prepared using 70% agglomerates and 30% acetaminophen, a poorly compressible drug, and were subjected toin vitrodrug release study. Amounts of the drug released at the end of 60 min (Y60), 300 min (Y300) and 480 min (Y480) were selected as dependent variables in a simplex lattice design. Batch IH05 that contained lactose and calcium hydrogen phosphate dihydrate in a 1:2 ratio could control the release for 12 hours and thus form the basis for twice a-day-dosing.

scholarly journals A New Calcium Oral Controlled-Release System Based on Zeolite for Prevention of Osteoporosis

Nutrients ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 2467 ◽  
Author(s):  
Angela Fabiano ◽  
Anna Maria Piras ◽  
Vincenzo Calderone ◽  
Lara Testai ◽  
Lorenzo Flori ◽  
...  
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Calcium Ions ◽  
Rank Order ◽  
In Vivo Studies ◽  
Current Therapy ◽  
Effective Prevention ◽  
Prevention Of Osteoporosis

Osteoporosis, a systemic skeleton disease, can be prevented by increasing calcium levels in serum via administration of calcium salts. However, traditional calcium-based formulations have not appeared to be effective, hence the purpose of the present work has been to prepare and test in vitro/vivo a formulation able to gradually release calcium during transit over the GI tract, thus increasing bioavailability and reducing daily dose, and hence, side effects. Calcium controlled-release granules based on zeolite and Precirol® were prepared. In the best case, represented by granules sized 1.2 mm, containing 20% Precirol®, 19% zeolite, 60% calcium (granule), the release lasted ≈6 h. The release is controlled by diffusion of calcium ions through the aqueous channels forming within granules, once these come into contact with physiological fluids. Such a diffusion is hindered by the interaction of calcium ions with the negatively charged surface of the zeolite. Ovariectomy was used to make rats osteopenic. For in vivo studies, rats were divided into the following groups. Sham: not treated; ova: ovariectomized (ova); CaCl2 1.0 g: ova, treated with 1.0 g/die Ca2+; CaCl2 0.5 g: ova, treated with 0.5 g/die Ca2+; granule 1.0 g, or granule 0.5 g: ova, treated with granules equivalent to 1.0 g/die or 0.5 g/die Ca2+ in humans. Ca2+ amounts in femur bone and bone marrow, femur mechanical characteristics, and femur medullary canalicule diameter were measured and the same efficacy rank order was obtained: ova < CaCl2 0.5 g < CaCl2 1.0 g < granule 0.5 g ≈ granule 1.0 g ≈ sham. The results show promise of an effective prevention of osteoporosis, based on a controlled-rate administration of a calcium dose half that administered by the current therapy, with reduced side effects.

scholarly journals PHARMACOKINETIC STUDY OF MATRIX MEMBRANE MODERATED TRANSDERMAL SYSTEM OF BOSENTAN MONOHYDRATE

2017 ◽  
Vol 10 (9) ◽  
pp. 255
Author(s):  
Revathi Mannam ◽  
Indira Muzib Yallamalli
Keyword(s):  
Controlled Release ◽  
High Performance ◽  
Release Kinetics ◽  
Research Work ◽  
Fold Increase ◽  
Oral Route ◽  
Fickian Diffusion ◽  
Pharmacokinetic Studies ◽  
The Matrix

Objective: The objective of the present research work is to carry out the pharmacokinetic studies of optimized matrix membrane moderatedtransdermal patch of bosentan monohydrate.Materials and Methods: The matrix membrane moderated transdermal system was formulated using HPMC, HPMC K4M and E RLPO. In vitrodiffusion studies were carried out using modified Franz diffusion cell and for the optimized transdermal patch, pharmacokinetic studies were carriedout using New Zealand male rabbits. Plasma samples were quantified using high-performance liquid chromatography.Results: The in vitro diffusion studies revealed that formulation F3 with HPMC K4M and E RLPO had controlled release up to 28 hrs, and a maximumof 95.02±2.68% drug was released. The release kinetics followed mixed order non-Fickian diffusion. The pharmacokinetic studies of the optimizedpatch revealed controlled release up to 45 hrs where a 2.2-fold increase in area under curve (AUC) and 3.8 times increase in mean residence time(MRT) were observed compared to oral route. The results were appeared to be significant at p≤0.05. The variation in half-life was found to be notstatistically significant when compared between oral and transdermal routes.Conclusion: The pharmacokinetic results concluded that the matrix membrane moderated transdermal system with extended AUC and MRT canenhance the bioavailability of bosentan monohydrate by minimizing the drug-related side effects in oral route.

The Permeability of Poly(lactic-co-glycolic acid) Nanoparticles Loaded with Psoralen to Human Skin in Medical Chemotherapy

2020 ◽  
Vol 12 (2) ◽  
pp. 163-169
Author(s):  
Liangming Li ◽  
Aihua Yang
Keyword(s):  
Side Effects ◽  
Human Skin ◽  
Plga Nanoparticles ◽  
Transdermal Drug Delivery System ◽  
Franz Diffusion Cell ◽  
Clinical Methods ◽  
Solvent Replacement ◽  
Polymer Deposition ◽  
Laser Confocal Microscope

Objective: In order to improve the clinical efficacy and reduce the side effects, PLGA nanoparticles loaded with psoralen for external use were prepared, and the permeation, distribution and influencing factors of PLGA nanoparticles delivered via microneedles in human skin were investigated. Methods: The psoralen nanoparticles were prepared by solvent replacement and interfacial polymer deposition. The percutaneous process of PLGA nanoparticles loaded with psoralen was observed with Franz diffusion cell and laser confocal microscope. The distribution of the nanoparticles in each cortex was quantified by HPLC. Results: The retention of PLGA nanoparticles delivered via microneedles in the skin was significantly increased (P < 0.01), and the retention in the epidermis was greater than that in the dermis (P < 0.01); the release rate in vitro was 75.58% after 24 hours, and less than 0.5% after 48 hours. Conclusion: PLGA nanoparticles loaded with psoralen can effectively promote the penetration and distribution of PLGA nanoparticles in human skin after being delivered to human skin through microneedles. With the increase of depth, the amount of PLGA nanoparticles gradually decreases, and with the extension of time, the penetration promotion effect of microneedles is more obvious. PLGA nanoparticles loaded with psoralen may become one of the clinical methods to improve the photochemotherapy of psoralen and develop a new transdermal drug delivery system to reduce its toxic and side effects.

scholarly journals Biodegradable Polymersomes for the Delivery of Gemcitabine to Panc-1 Cells

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Nimil Sood ◽  
Walter T. Jenkins ◽  
Xiang-Yang Yang ◽  
Nikesh N. Shah ◽  
Joshua S. Katz ◽  
...  
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Chemotherapeutic Agent ◽  
Therapeutic Index ◽  
Drug Bioavailability ◽  
Anticancer Chemotherapy ◽  
Poly Ethylene Oxide ◽  
Poly Ethylene ◽  
Poly Caprolactone

Traditional anticancer chemotherapy often displays toxic side effects, poor bioavailability, and a low therapeutic index. Targeting and controlled release of a chemotherapeutic agent can increase drug bioavailability, mitigate undesirable side effects, and increase the therapeutic index. Here we report a polymersome-based system to deliver gemcitabine to Panc-1 cells in vitro. The polymersomes were self-assembled from a biocompatible and completely biodegradable polymer, poly(ethylene oxide)-poly(caprolactone), PEO-PCL. We showed that we can encapsulate gemcitabine within stable 200 nm vesicles with a 10% loading efficiency. These vesicles displayed a controlled release of gemcitabine with 60% release after 2 days at physiological pH. Upon treatment of Panc-1 cells in vitro, vesicles were internalized as verified with fluorescently labeled polymersomes. Clonogenic assays to determine cell survival were performed by treating Panc-1 cells with varying concentrations of unencapsulated gemcitabine (FreeGem) and polymersome-encapsulated gemcitabine (PolyGem) for 48 hours. 1 μM PolyGem was equivalent in tumor cell toxicity to 1 μM FreeGem, with a one log cell kill observed. These studies suggest that further investigation on polymersome-based drug formulations is warranted for chemotherapy of pancreatic cancer.

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