Stereomicroscopic Imaging Technique for the Quantification of Cold Flow in Drug-in-Adhesive Type of Transdermal Drug Delivery Systems

Krishnaiah, Y. S. R.; Katragadda, Usha; Khan, Mansoor A.

doi:10.1002/jps.23915

Cited by 9 publications

(4 citation statements)

References 15 publications

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“…The prepared patch was placed at room temperature for 48 h, and then the cold flow experiment was performed. 14 The film was cut into a round patch 1.2 cm in diameter, and the liner film was torn off and attached to the 4 × 4 cm release liner of the nonfluoropolymer coating, and then the release liner was placed on top with the surface of the fluoropolymer coating inside. The top and bottom release lines were then carefully taped together to prevent lateral movement of the samples during cold flow.…”

Section: Adhesion Properties Of Patchesmentioning

confidence: 99%

“…Plasticization occurs after the PSA has been loaded with drug and can disrupt the cohesion of the PSA, resulting in DIA leaking from the TDDS (cold flow) edge under the backing membrane, leading to storage problems, adhesion failure, and the formation of a dark ring on skin application. , Several reports of the dark ring phenomenon have been received by the United States Food and Drug Administration (FDA) . This has serious implications for the safety and efficacy of the product. − Therefore, the United States Pharmacopeia and the National Formulary include the cold flow test as a specific quality test for topical and transdermal drug products …”

Section: Introductionmentioning

confidence: 99%

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3-Methacryloxypropyltrimethoxysilane-Modified Hydroxyl Acrylate Pressure-Sensitive Adhesive with High Antiplasticity for Efficient Transdermal Drug Delivery

Wang,

Nan,

Song

et al. 2024

ACS Appl. Polym. Mater.

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In transdermal patches, pressure-sensitive adhesives (PSAs) are considered the most critical excipients due to their ability to provide adhesion and act as a drug reservoir. However, the loaded drugs plasticize the patches, resulting in a cold flow phenomenon, which poses a product safety risk and reduces treatment efficacy. Herein, 3-methacryloxypropyltrimethoxysilane (KH-570)-modified hydroxyl acrylate PSA (AAOK) was proposed. Diclofenac, ketoprofen, tulobuterol, and oxybutynin were selected as model drugs. The results showed that when not loaded with drugs, the performance of AAOK was not significantly different from that of hydroxyl acrylate PSA (AAOH). Interestingly, when loaded with drugs, AAOK automatically forms a cross-linked system through drug catalysis, which exerts a strong antiplasticity without reducing the ability of AAOK to load and deliver the drug. Specifically, the shear strength of drug-loaded AAOK increased by more than 10-fold compared to AAOH. The cold flow area of drug-loaded AAOK was reduced by more than 15-fold compared to commercial DURO-TAK 87-2287. In addition, the "dark ring" phenomenon was not observed with AAOK compared to that with DURO-TAK 87-2287 on the human forearm after drug loading. After loading four model drugs into AAOK, a high drug loading and efficient drug delivery were endowed for AAOK in vitro and in vivo. The molecular mechanism for the improved antiplasticity of the drug-loaded AAOK was that the drug molecules had a catalyzing effect on the self-condensation reactions of KH-570. This study opens up ideas for the investigation of transdermal patches with high antiplasticity and efficient transdermal application.

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Section: Adhesion Properties Of Patchesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

3-Methacryloxypropyltrimethoxysilane-Modified Hydroxyl Acrylate Pressure-Sensitive Adhesive with High Antiplasticity for Efficient Transdermal Drug Delivery

Wang,

Nan,

Song

et al. 2024

ACS Appl. Polym. Mater.

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“…Cold flow was measured by microscopical method by viewing the patch under microscope at initial and after 1-month, when stored at 40°C/ 75% RH. [20][21][22]…”

Section: Cold Flow Study Of Rotigotine Patchmentioning

confidence: 99%

Formulation Development of Rotigotine Transdermal System Using Dot-Matrix Technology

Prajapati¹,

Mandli

2020

Int. J. Pharm. Sci. Drug Res.

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The purpose of this research was to prepare and evaluate drug-in-adhesive type patches of rotigotine using dot-matrix technology, which is the new generation of drug-in-adhesive transdermal delivery system (TDS) that deliver drug therapy through less patch surface area and without compromising adhesion. Preformulation studies, like solubility in permeation enhancers, compatibility study, transmission study, uptake study, and crystallization study of rotigotine in various pressure-sensitive adhesive (PSA) polymers were performed. Transdermal system was prepared by solvent casting method. Central composite design (CCD) was chosen for optimization of the formulation. Design of experiment (DoE) was used to study the impact of critical formulation parameters, like silicone adhesive concentration, povidone K29/32 concentration, and propylene glycol concentration. Crystallization study of rotigotine in different PSAs suggested that crystal inhibitor is required to load drugs above 5%. Selection of optimum batch was made using a constraint-based graphical optimization technique. The optimum batch exhibited desired in vitro adhesion parameters, like peel, tack, shear, and permeation rate, which is suitable for 3 days’ wear properties and desired permeation rate. The optimum batch was evaluated for appearance, weight of matrix, thickness, % assay of drug content, in vitro adhesion testing, cold flow study, and ex vivo skin permeation studies. Backing film Scotchpak 9730 and release liner Scotchpak-1022 was selected based on transmission and uptake study of rotigotine. Stability study indicates that developed formulation remains stable. The present research confirms the feasibility of developing rotigotine transdermal system using novel technology.

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“…Therefore, to fulfill the research gap as mentioned above, this study aimed to develop a versatile IA tool for investigating the wetting properties, gel formation and erosion rate of eutectic effervescent tablets under a stereomicroscope with the IA technique. Typically, the stereomicroscope is employed to observe the morphology of pharmaceutical dosage forms such as granules [29], the microneedle patch [30] or to monitor the physical change in formulation in the transdermal drug delivery system [31]. In this study, the stereomicroscope was used to capture morphological change during immersion in a medium and, quantitative data including the rate of wetting, gel formation and erosion were extrapolated from the image sequence using OLYMPUS Stream Basic 2.2 which is an image processing program.…”

Section: Introductionmentioning

confidence: 99%

Stereomicroscope with Imaging Analysis: A Versatile Tool for Wetting, Gel Formation and Erosion Rate Determinations of Eutectic Effervescent Tablet

2022

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Wettability, gel formation and erosion behaviors could influence the drug release pattern of solid dosage forms. Typically, these parameters are evaluated using a variety of techniques. Nonetheless, there has been no previous research on versatile tool development for evaluating several tablet characteristics with a single tool. The aim of this study was to develop the versatile tool for measuring various physical properties of eutectic effervescent tablets and also investigate the relationship between these parameters with parameters from drug dissolution. Ibuprofen (IBU)-poloxamer 407 (P407) eutectic effervescent tablets were fabricated with a direct compression method. Their wetting properties, gel formation and erosion behaviors were investigated using a stereomicroscope with imaging analysis in terms of the liquid penetration distance, gel thickness and erosion boundary diameter, respectively. In addition, the dissolution rate (k) and disintegration time of eutectic effervescent tablets in 0.1 N HCl buffer pH 1.2 were also determined. Incorporation of P407 into the IBU tablet improved the tablet wetting properties with increasing liquid penetration distance under stereoscope. CO2 liberation from effervescent agents promoted tablet surface roughness from matrix erosion. The relationship between observed physical properties and disintegration and dissolution parameters suggested that the combination of erosion by effervescent agents and gel formation by P407 had a potential influence on dissolution enhancement of the formulation. Therefore, a developed stereomicroscope with an imaging analysis technique was exhibited as an alternative versatile tool for determining the wetting properties, gel formation and erosion behaviors of pharmaceutical solid dosage forms.

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Stereomicroscopic Imaging Technique for the Quantification of Cold Flow in Drug-in-Adhesive Type of Transdermal Drug Delivery Systems

Cited by 9 publications

References 15 publications

3-Methacryloxypropyltrimethoxysilane-Modified Hydroxyl Acrylate Pressure-Sensitive Adhesive with High Antiplasticity for Efficient Transdermal Drug Delivery

3-Methacryloxypropyltrimethoxysilane-Modified Hydroxyl Acrylate Pressure-Sensitive Adhesive with High Antiplasticity for Efficient Transdermal Drug Delivery

Formulation Development of Rotigotine Transdermal System Using Dot-Matrix Technology

Stereomicroscope with Imaging Analysis: A Versatile Tool for Wetting, Gel Formation and Erosion Rate Determinations of Eutectic Effervescent Tablet

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