FORMULATION DEVELOPMENT AND CHARACTERIZATION OF TRIAMCINOLONE LOADED CUBOSOMES FOR TRANSDERMAL DRUG DELIVERY

Psoriasis is a chronic condition that is caused by the negative signals given by immune system, which leads to hyperproliferation and other inflammatory reactions on the skin. These conditions may adversely affect the quality of the patient’s life leading to psychological stress. Topical delivery of drug is always preferred for Psoriasis because other treatments may lead to systemic intoxication and other adverse reactions. Triamcinolone is a topical corticosteroid belonging to BCS class IV (low solubility and permeability) used to treat Psoriasis. The limitations with transdermal delivery is that only a small amount of the drug can be transferred through the skin tissue due to the barrier effects of the Stratum corneum. Therefore, Novel transdermal delivery system, Cubosomes belonging to Nanostructured lipid carriers were chosen to overcome the issues of solubility and permeability. Twelve formulations were prepared with various ratios of Glyceryl monooleate (2.5 to 5%) & Poloxamer 407 (0.5 to 2%) and the formulations were evaluated for particle size, PDI, zeta potential, entrapment efficacy, drug content and in-vitro release. The best composition of Cubosomes was selected and incorporated into transdermal patch and the formulated patches were evaluated.

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Formulation development and in-vitro characterisation of ethosomes for the enhanced transdermal delivery of clotrimazole

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v10i2.270 ◽

2019 ◽

Vol 10 (2) ◽

pp. 874-882

Author(s):

Vidya Viswanad ◽

Anju PG ◽

Gopika S Kumar ◽

Sivapriya G Nair

Keyword(s):

Transdermal Delivery ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Clinical Effectiveness ◽

Permeation Rate ◽

Formulation Development ◽

Preparation Conditions ◽

Two Factors ◽

Vitro Release

The target of the study was the development and in vitro characterisation of an effective ethosomal formulation of clotrimazole and to the performance of the formulation was investigated under different preparation conditions. The EE and from 9 formulations, the optimisation was done on the basis of its results which considering the concentration of lecithin and ethanol as the two factors and EE and in vitro release as their responses. The optimization was done on the basis of its results which considering the concentration of lecithin and ethanol as the two factors and EE and in vitro release as their responses. F6 formulation gained a very good release of drug and highest entrapment efficiency of 93.203%. The results of permeation flux were obtained in the order of MLVs > ESUVs > SSUVs > LUVs. This study gives an idea about the vesicles structure and the size, the technique used, the drug EE and the permeation rate. They were taking the above factors into consideration results in improving clinical effectiveness in transdermal delivery of an ethosomal formulation of clotrimazole.

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Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.3.6 ◽

2011 ◽

Vol 4 (3) ◽

pp. 1477-1483

Author(s):

Natarajan R ◽

N Patel ◽

Rajendran N N ◽

M Rangapriya

Keyword(s):

Antihypertensive Drugs ◽

In Vitro Release ◽

Immediate Release ◽

Wet Granulation ◽

Physical Parameters ◽

Dissolution Profile ◽

Formulation Development ◽

Sodium Starch Glycolate ◽

Bilayer Tablets

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.

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Characterization of α-melanocyte-stimulating hormone (α-MSH)-like peptides in discrete regions of the rat brain. In vitro release of α-MSH from perifused hypothalamus and amygdala

Brain Research ◽

10.1016/0006-8993(90)90471-m ◽

1990 ◽

Vol 513 (2) ◽

pp. 299-307 ◽

Cited By ~ 12

Author(s):

Denis Tranchand Bunel ◽

Catherine Delbende ◽

Catherine Blasquez ◽

Sylvie Je´gou ◽

Hubert Vaudry

Keyword(s):

Rat Brain ◽

In Vitro Release ◽

Melanocyte Stimulating Hormone ◽

Vitro Release ◽

Stimulating Hormone

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Preparation and characterization of fentanyl-loaded PLGA microspheres: in vitro release profiles

International Journal of Pharmaceutics ◽

10.1016/s0378-5173(01)00968-1 ◽

2002 ◽

Vol 234 (1-2) ◽

pp. 195-203 ◽

Cited By ~ 62

Author(s):

Hak Soo Choi ◽

Sun-Ah Seo ◽

Gilson Khang ◽

John M. Rhee ◽

Hai Bang Lee

Keyword(s):

In Vitro Release ◽

Plga Microspheres ◽

Vitro Release ◽

Release Profiles

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Formulation and Evaluation of Transdermal patch of Methimazole

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00811 ◽

2021 ◽

pp. 4667-4672

Author(s):

Nani Tadhi ◽

Himansu Chopra ◽

Gyanendra Kumar Sharma

Keyword(s):

Drug Release ◽

Release Kinetics ◽

In Vitro Release ◽

Transdermal Patch ◽

Formulation Development ◽

In Vitro Drug Release ◽

Drug Release Study ◽

Percent Moisture ◽

Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

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Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/j34880 ◽

2010 ◽

Vol 13 (2) ◽

pp. 286 ◽

Cited By ~ 13

Author(s):

Tailane Sant´Anna Moreira ◽

Valéria Pereira De Sousa ◽

Maria Bernadete Riemma Pierre

Keyword(s):

Oleic Acid ◽

Rheological Behavior ◽

Transdermal Delivery ◽

In Vitro Release ◽

Delivery Systems ◽

Penetration Enhancer ◽

Release Studies ◽

Vitro Release ◽

Gel Transition

Abstract PURPOSE: Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (Tsol-gel) were also carried out in these systems. METHODS: In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm2) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm2. h -1. The determination of viscosity was carried out at different shear rates (γ) between 0.1- 1000 S-1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine Tsol-gel. RESULTS: Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% compared to other concentrations of the penetration enhancer. Tsol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. CONCLUSIONS: Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics. Novelty of the work: A transdermal delivery of non-steroidal antinflammatory drugs like lumiracoxib (LM) can be an interesting alternative to the oral route of this drug, since it was recently withdraw of the market due to the liver damage when systemically administered in tablets as dosage form. There are no transdermal formulations of LM and it could be an alternative to treat inflammation caused by arthritis or arthrosis. Then, an adequate delivery system to LM is necessary in order to release the drug properly from the PBDS as well as have good characteristics related to semi-solid preparations for transdermal application, which were evaluated through in vitro release studies and rheological behavior in this paper, respectively.

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Preclinical Evidence of Nanomedicine Formulation to Target Mycobacterium tuberculosis at Its Bone Marrow Niche

Pathogens ◽

10.3390/pathogens9050372 ◽

2020 ◽

Vol 9 (5) ◽

pp. 372 ◽

Cited By ~ 1

Author(s):

Jaishree Garhyan ◽

Surender Mohan ◽

Vinoth Rajendran ◽

Rakesh Bhatnagar

Keyword(s):

Bone Marrow ◽

Mycobacterium Tuberculosis ◽

In Vitro Release ◽

Bone Marrow Niche ◽

Mice Model ◽

Latently Infected ◽

Marrow Mesenchymal Stem Cells

One-third of the world’s population is estimated to be latently infected with Mycobacterium tuberculosis (Mtb). Recently, we found that dormant Mtb hides in bone marrow mesenchymal stem cells (BM-MSCs) post-chemotherapy in mice model and in clinical subjects. It is known that residual Mtb post-chemotherapy may be responsible for increased relapse rates. However, strategies for Mtb clearance post-chemotherapy are lacking. In this study, we engineered and formulated novel bone-homing PEGylated liposome nanoparticles (BTL-NPs) which actively targeted the bone microenvironment leading to Mtb clearance. Targeting of BM-resident Mtb was carried out through bone-homing liposomes tagged with alendronate (Ald). BTL characterization using TEM and DLS showed that the size of bone-homing isoniazid (INH) and rifampicin (RIF) BTLs were 100 ± 16.3 nm and 84 ± 18.4 nm, respectively, with the encapsulation efficiency of 69.5% ± 4.2% and 70.6% ± 4.7%. Further characterization of BTLs, displayed by sustained in vitro release patterns, increased in vivo tissue uptake and enhanced internalization of BTLs in RAW cells and CD271+BM-MSCs. The efficacy of isoniazid (INH)- and rifampicin (RIF)-loaded BTLs were shown using a mice model where the relapse rate of the tuberculosis was decreased significantly in targeted versus non-targeted groups. Our findings suggest that BTLs may play an important role in developing a clinical strategy for the clearance of dormant Mtb post-chemotherapy in BM cells.

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Synthesis, characterization of dextran hydrogels and their in vitro release of gentamycin sulphate

Journal of Applied Biomaterials & Functional Materials ◽

10.5301/jabfm.5000233 ◽

2015 ◽

Vol 13 (3) ◽

pp. 0-0 ◽

Cited By ~ 1

Author(s):

Rui Guo ◽

Peizhe Chen ◽

Yunfei Mo ◽

Yong Lan ◽

Wei Xue ◽

...

Keyword(s):

In Vitro Release ◽

Vitro Release

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Preparation and characterization of domperidone nanoparticles for dissolution improvement

Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) ◽

10.31351/vol27iss1pp39-52 ◽

2018 ◽

Vol 27 (1) ◽

pp. 39-52

Author(s):

Mohammed Sabar Al-lami ◽

Malath H. Oudah ◽

Firas A. Rahi

Keyword(s):

Particle Size ◽

Average Particle Size ◽

In Vitro Release ◽

Methyl Cellulose ◽

Precipitation Method ◽

Average Particle ◽

Antisolvent Precipitation ◽

Stirring Time

This study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p? 0.05) effect on particle size. The best formula was obtained with lowest average particle size of 84.05. This formula was studied for compatibility by FTIR and DSC, surface morphology by FESEM and crystalline state by XRPD. Then domperidone nanoparticles were formulated into a simple capsule dosage form in order to study of the in vitro release of drug from nanoparticles in comparison raw drug and mixture of polymer:drug ratios of 2:1. The release of domperidone from best formula was highly improved with a significant (p? 0.05) increase.

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