In Vitro and In Vivo Assessment of Matrix Type Transdermal Therapeutic System of Labetalol Hydrochloride

Mittal, Ashu; Parmar, Shikha; Singh, Bhugwan

doi:10.2174/156720109789941614

Cited by 10 publications

(5 citation statements)

References 22 publications

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“…To evaluate the efficiency of the patches, a folding endurance test was performed. The folding endurance value of each patch was accomplished by rapid folding and unfolding of the patch at the point of breakage [ 20 ]. When a patch was folded and unfolded several times in quick succession at the same point without breaking, it defined the folding endurance value.…”

Section: Methodsmentioning

confidence: 99%

Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery

et al. 2021

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Transdermal drug delivery is important to maintain plasma drug concentrations for therapeutic efficacy. The current study reports the design, formulation, and evaluation of tizanidine transdermal patches formulated using chitosan and thiolated chitosan, ethyl cellulose (EC), polyvinylpyrrolidone (PVP), and Eudragit RL100 in different ratios. The tizanidine patches were formulated using flaxseed oil and coriander oil in the concentrations of 1% v/w, 2% v/w, 3% v/w, 4% v/w, 5% v/w, and 10% v/w. The patches were subjected to characterization of physicochemical property (thickness, weight uniformity, drug content, efficiency, percentage moisture uptake/loss), in vitro drug release and drug permeation, skin irritation, in vivo application, pharmacokinetics analysis, and stability studies. The results indicate that the interaction of thiolated chitosan with the negative charges of the skin opens the tight junctions of the skin, whereas flaxseed and coriander oils change the conformational domain of the skin. The novelty of this study is in the use of flaxseed and coriander oils as skin permeation enhancers for the formulation of tizanidine transdermal patches. The formulations follow non-Fickian drug release kinetics. The FTZNE23, FTZNE36 and FTZNE54, with 5% v/w flaxseed oil loaded formulations, exhibited higher flux through rabbit skin compared with FTZNE30, FTZNE35, FTZNE42, and FTZNE47, formulations loaded with 10% v/w coriander oil. The study concludes that flaxseed oil is a better choice for formulating tizanidine patches, offering optimal plasma concentration and therapeutic efficacy, and recommends the use of flaxseed and coriander oil based patches as a novel transdermal delivery system for tizanidine and related classes of drugs.

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Section: Methodsmentioning

confidence: 99%

Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery

et al. 2021

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“…Add required quantity of drug mixed and well. After that final volume was made up to 50 ml with distilled water 4 . …”

Section: Preparation Of In Situ Gelling Solution Of Valacyclovirmentioning

confidence: 99%

Floating in-Situ Gelling System for Stomach Specific Oral Drug Delivery of Valacyclovir

Patel¹,

Gandhi²,

Shah³

2017

Int. Res. J. Pharm.

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The present investigation deals with the formulate and evaluate oral in situ floating drug delivery system for Valacyclovir which undergoes ion dependent sol -gel transition at gastric physiological conditions, thereby prolonging the retention of the system in stomach. Sodium alginate as gelling agent whose gelation is triggered by source of Calcium ions in the form of calcium carbonate. The study demonstrates the feasibility of prolonging gastric residence time and release rate of Valacyclovir by preparing floating in situ gel system using ion-cross linking in situ gel forming polymers. The formulated batches were further studied for Floating lag time, Gelling lag time, Viscosity and in vitro drug release was carried out. The prepared floating oral in situ gel formulation was optimized using 3 2 full factorial experimental design. Floating oral in situ gel formulation optimized for amount of sodium alginate(X1) and amount of calcium carbonate(X2) independent variables) in order to achieve desired response of floating lag time(Y1), viscosity(Y2), %CDR at 1 hour(Y3) and %CDR at 8 hour(Y4)(dependent variables). The experimental results of optimized batch (F6) revealed that floating lag time = 54 sec, viscosity = 218 cP, 39.83 %CDR = 1hour and 88.96 %CDR = 8 hour. The improved characteristics of the selected floating oral in situ gel system make them excellent candidates for gastric retention.

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“…A strip of Patch of specific surface area (2 cm 2 ) was cut and folded repeatedly at one place till it broke. The number of times the patch was folded before breaking at the same place represented folding endurance [17,18].…”

Section: Folding Endurancementioning

confidence: 99%

Formulation and Evaluation of Nateglinide Patches for Transdermal Drug Delivery.

Solunke¹,

Chaudhari²

2017

JCPR

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Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. Nateglinide is an Anti-Diabetic drug with a shorter half life, low bioavailability up to 72 % undergoes extensive first pass metabolism are required to maintain the therapeutic level it has chosen as transdermal drug delivery system. The present study was to formulate and evaluate transdermal drug delivery system of Nateglinide using polymers such as HPMC & Eudragit RL100 by solvent casting technique. The prepared formulations were evaluated for different physicochemical characteristics like Weight Variation, Folding Endurance, Flatness, pH of patches, % Moisture Content, % Moisture uptake, % Elongation, % Drug Content & % Drug Release. The drug release characteristics of the formulation were studied in-vitro by using semi-permeable membrane. The in-vitro drug release plot has shown that the drug release followed zero order kinetics & Higuchi model, which was evidenced from the regression values. Based on the drug release and physicochemical values obtained from the formulation F 7 is considered as an optimized formulation which shows higher percentage of drug release (96.27±0.68 % at 14 hour) with diffusion mediated mechanism. Korsmeyer-Peppas exponential plots shows fairly linear & it is well supported by their regression coefficients values & slope value (n) were >1 which suggest that drug was released by Super Case-II transport.

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In Vitro and In Vivo Assessment of Matrix Type Transdermal Therapeutic System of Labetalol Hydrochloride

Abstract: The above TTS holds promise for improved bioavailability and better management of hypertension on long term basis.

Cited by 10 publications

References 22 publications

Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery

Fabrication of Tizanidine Loaded Patches Using Flaxseed Oil and Coriander Oil as a Penetration Enhancer for Transdermal Delivery

Floating in-Situ Gelling System for Stomach Specific Oral Drug Delivery of Valacyclovir

Formulation and Evaluation of Nateglinide Patches for Transdermal Drug Delivery.

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