scholarly journals Development of Tizanidine HCl transdermal patches: In-vitro and Ex-vivo characterization

2019 ◽  
Vol 9 (1-s) ◽  
pp. 295-300
Author(s):  
Dr. Shayeda ◽  
Nusrat Ayesha
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Transdermal Patches ◽  
Ex Vivo Permeation ◽  
Release Studies ◽  
Transdermal Drug Delivery Systems ◽  
Folding Endurance ◽  
Vitro Release

The purpose of this work was to design and evaluate matrix type transdermal patches of Tizanidine hydrochloride using Hypromellose (HPMC E15) as polymer, dibutyl phthalate as plasticizer and citral as permeation enhancer. The DSC and FTIR results showed the compatibility of the excipients with the drug. These transdermal drug delivery systems were characterized for their thickness, folding endurance, content uniformity, tensile strength and in-vitro release studies of the drug from the polymeric matrix. In-vitro release studies and ex-vivo permeation were carried out with modified Franz diffusion cell using pH 5.8 & pH 7.4 phosphate buffers as receptor medium and it showed controlled release of drug. The results suggest that the formulation of TIZ may be useful in the development of a therapeutic system to deliver TIZ across the skin for a prolonged period, i.e. 24 hr. Keywords: Tizanidine Hydrochloride, Transdermal patch, HPMC E15, in-vitro & ex-vivo.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF PANTOPRAZOLE SODIUM

2021 ◽  
pp. 287-291
Author(s):  
M. R. SHIVALINGAM ◽  
ARUL BALASUBRAMANIAN ◽  
KOTHAI RAMALINGAM
Keyword(s):  
In Vitro Release ◽  
Skin Permeability ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Prolonged Release ◽  
Peptic Ulcers ◽  
Transdermal Patches ◽  
Release Studies ◽  
Vitro Release

Objective: The present study was an attempt to develop an alternative dosage form for the existing conventional oral, parenteral proton pump inhibitor (PPI) as transdermal patches for treating peptic ulcers. Methods: Transdermal patches of PPI were prepared using HPMC E5 with PVP K 30 and HPMC E5 with Eudragit L100 polymers in different ratios by a solvent evaporation method. All the formulated patches were subjected to various evaluation parameters such as thickness, folding endurance, weight uniformity, content uniformity, swelling index, percentage moisture content, moisture uptake, surface pH and in vitro release studies. Results: All patches exhibited satisfactory characteristics regarding integrity, flexibility, dispersion of drug, and other quality control parameters. In the in vitro release studies of transdermal patches, formulation F1 showed the prolonged release of drug (98.99 %) for 24 h, which indicates the maximum availability of the drug, and the in vitro skin permeability studies also showed that 96.26 % of drug Pantoprazole sodium permeated through the rat abdominal skin in 24 h. The kinetic studies were carried out and it was found that all the formulations follow zero-order and the release mechanism of drugs was found to be diffusion rate-limited, Non-Fickian mechanism which was confirmed by Korsmeyer–Peppas model. Conclusion: This suggests the transdermal application of Pantoprazole sodium holds the promised controlled release of the drug for an extended period of time.

Sodium alginate nanoparticles as a new transdermal vehicle of glucosamine sulfate for treatment of osteoarthritis

2017 ◽  
Vol 9 (3-4) ◽  
Author(s):  
Asmaa S. El-Houssiny ◽  
Azza A. Ward ◽  
Dina M. Mostafa ◽  
Salwa L. Abd-El-Messieh ◽  
Kamal N. Abdel-Nour ◽  
...  
Keyword(s):  
Side Effects ◽  
Surface Charge ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Glucosamine Sulfate ◽  
Suspension Stability ◽  
Rat Skin ◽  
Release Studies ◽  
Vitro Release

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.

Nanostructured Lipid Carriers for Intranasal Administration of Olanzapine in the management of Schizophrenia

2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Poloxamer 407 ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Vitro Release

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.

scholarly journals FORMULATION AND EVALUATION OF A CHITOSAN-PVA-GELLAN INSULIN IMPLANT

2017 ◽  
Vol 9 (3) ◽  
pp. 37
Author(s):  
Satish C. S.
Keyword(s):  
Diffusion Coefficient ◽  
Insulin Release ◽  
In Vitro Release ◽  
Poly Vinyl Alcohol ◽  
Content Uniformity ◽  
Release Studies ◽  
Solution Casting Method ◽  
Implant System ◽  
Vitro Release

Objective: The purpose of this study was to ascertain the applicability of degradable materials for fabrication of an insulin release system.Methods: Insulin implants were prepared by using poly (vinyl alcohol) (PVA), gellan and chitosan by solution casting method. The prepared implants were evaluated for swellability, content uniformity, potency and purity of insulin in implants, scanning electron microscopy studies, in vitro release studies, in vitro degradation studies using lysozyme, stability studies and circular dichroism spectroscopy.Results: The swelling degree of the implants was found to be in the range of 1.07-1.56. The diffusion coefficient of water through the implant was found to depend on the calcium chloride (CaCl2) concentration. The diffusion coefficient of insulin through the chitosan-PVA-gellan in the early stages was found to be in the range of 1.99´10-5 cm2/sec to 5.24´10-5 cm2/sec and at later stages in the range of 6.9´10-6 cm2/sec to 1.10´10-5 cm2/sec. The weight of the implants was 48±0.58 mg. The insulin content in the implants was 9.86±0.10 mg. The potency of insulin extracted from the implants was 27.11±0.75 U/mg or 95.12±2.61 % of the control insulin. The in vitro release studies showed that insulin was released completely in a period of 13-19 d depending on the composition of the implant. The increase in CaCl2 retarded the rate of insulin release whereas the increase in PVA content leads to the rapid release of insulin. The device was found to undergo significant weight loss due to enzyme mediated degradation.Conclusion: These studies provide validity for the potential utility of chitosan-PVA-gellan implant systems for the delivery of insulin. The studies also demonstrate that insulin maintained its integrity within the implant system. Implants showed the complete release of insulin in 19 d and the release of insulin from the implants depended on the amount of CaCl2.

scholarly journals Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3455
Author(s):  
Muhammad Shahid Latif ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Sheikh Abdur Rashid ◽  
Md. Habibur Rahman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Transdermal Patches ◽  
Percent Moisture ◽  
Vitro Release

Transdermal drug delivery systems (TDDSs) have become innovative, fascinating drug delivery methods intended for skin application to achieve systemic effects. TDDSs overcome the drawbacks associated with oral and parenteral routes of drug administration. The current investigation aimed to design, evaluate and optimize methotrexate (MTX)-loaded transdermal-type patches having ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) at different concentrations for the local management of psoriasis. In vitro release and ex vivo permeation studies were carried out for the formulated patches. Various formulations (F1–F9) were developed using different concentrations of HPMC and EC. The F1 formulation having a 1:1 polymer concentration ratio served as the control formulation. ATR–FTIR analysis was performed to study drug–polymer interactions, and it was found that the drug and polymers were compatible with each other. The formulated patches were further investigated for their physicochemical parameters, in vitro release and ex vivo diffusion characteristics. Different parameters, such as surface pH, physical appearance, thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, skin irritation, stability and drug content uniformity, were studied. From the hydrophilic mixture, it was observed that viscosity has a direct influence on drug release. Among all formulated patches, the F5 formulation exhibited 82.71% drug release in a sustained-release fashion and followed an anomalous non-Fickian diffusion. The permeation data of the F5 formulation exhibited about a 36.55% cumulative amount of percent drug permeated. The skin showed high retention for the F5 formulation (15.1%). The stability study indicated that all prepared formulations had very good stability for a period of 180 days. Therefore, it was concluded from the present study that methotrexate-loaded transdermal patches with EC and HPMC as polymers at different concentrations suit TDDSs ideally and improve patient compliance for the local management of psoriasis.

scholarly journals Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 64 ◽  
Author(s):  
Lupe Carolina Espinoza ◽  
Marcelle Silva-Abreu ◽  
Beatriz Clares ◽  
María José Rodríguez-Lagunas ◽  
Lyda Halbaut ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Release Profile ◽  
In Vivo Models ◽  
Tablet Form ◽  
Ex Vivo Permeation ◽  
Vitro Release

Donepezil (DPZ) is widely used in the treatment of Alzheimer’s disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood–brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Composition of NE was established using three pseudo-ternary diagrams and PNE was developed by incorporating Pluronic F-127 to the aqueous phase. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined for both formulations. The tolerability was evaluated by in vitro and in vivo models. DPZ-NE and DPZ-PNE were transparent, monophasic, homogeneous, and physically stable with droplets of nanometric size and spherical shape. DPZ-NE showed Newtonian behavior whereas a shear thinning (pseudoplastic) behavior was observed for DPZ-PNE. The release profile of both formulations followed a hyperbolic kinetic. The permeation and prediction parameters were significantly higher for DPZ-PNE, suggesting the use of polymers to be an effective strategy to improve the bioadhesion and penetration of the drug through nasal mucosa, which consequently increase its bioavailability.

Improved in vitro Release and ex vivo Permeation of Zotepine as Microemulsion Gel Formulation through Transdermal Application

2021 ◽  
Vol 14 (1) ◽  
pp. 5343-5352
Author(s):  
Akhila Keshoju ◽  
Dinesh Suram ◽  
Chandra Mouli Golla ◽  
Nagaraj B
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Gelling Agent ◽  
Prolonged Release ◽  
Rat Skin ◽  
Skin Delivery ◽  
Ex Vivo Permeation ◽  
Vitro Release ◽  
Microemulsion Gel

Zotepine is atypical antipsychotic drug with poor oral bioavailability due to first-pass metabolism and poor aqueous solubility. The objective of the current investigation was preparation and ex vivo characterization of Zotepine (ZT) loaded microemulsion (ZT-ME) and microemulsion gel (ZT-MEG) for enhanced transdermal delivery.  ZT-ME formulation was prepared with 7.5% oleic acid, 30% w/v of Tween80 and 30%w/v of absolute ethanol as oil, surfactant and cosurfactant, respectively. Optimized ZT-ME formulation was selected and converted to ZT-MEG using carbopol as gelling agent. ZT-ME and ZT-MEG subjected to in vitro release and ex vivo permeation studies through rat skin, comparison with ZT coarse suspension (ZT-CS). ZT-ME formulation showed desirable physicochemical properties and stable with dilution stress. Prepared ZT-MEG formulation has showed better rheological behaviour and good spreadability. ZT-ME and ZT-MEG showed prolonged release compared with ZT-CS formulation over 24 h. ZT-ME and ZT-MEG exhibited 5-folds and 3.5-folds in permeation through rat skin compared with ZT-CS formulation. Overall, ZT-MEG formulation could be considered as an alternative delivery approach for enhanced skin delivery. 

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