Formulation optimization of a drug in adhesive transdermal analgesic patch

Ravula, Ranadheer; Herwadkar, Anushree; Abla, M. J.; Little, John W.; Banga, Ajay K.

doi:10.3109/03639045.2015.1071832

Cited by 12 publications

(5 citation statements)

References 28 publications

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“…The role played by permeation-enhancing agents in the transdermal delivery of drugs has been extensively investigated in the last few decades. In this context, the incorporation of such chemicals in DIA is demonstrated as a promising approach, which disrupts the skin membrane, overcomes the drug transport barriers and thereby improves the transdermal flux [47]. Consequently, to enhance the solubility, drug loading and the transdermal flux of pioglitazone, potent skin permeation enhancers were selected.…”

Section: Resultsmentioning

confidence: 99%

Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch

et al. 2019

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The administration of pioglitazone as an oral therapy is restricted due to various challenges. The aim of the current investigation was to evaluate the suitability of pioglitazone in adhesive transdermal patch as an alternative delivery system, in order to improve therapeutic delivery. Drug in adhesive pioglitazone (2% w/w) transdermal patch were optimized for drug release, suitable adhesive, and skin permeation enhancer. The selected patch was examined for drug-loading capacity and the patch with greater pioglitazone (6% w/w) was evaluated in rat models. The release of pioglitazone was influenced by the tested adhesive and was shown to be significantly higher (p < 0.001) with patch, prepared using Duro-Tak 87-2516. The ex vivo permeation results substantiate the release data as a greater transdermal flux (15.67 ± 2.35 µg/cm2/h) was demonstrated in patch fabricated with Duro-Tak 87-2516. Skin penetration enhancers promoted the ex vivo transdermal delivery of pioglitazone, and was ~2 folds (p < 0.0001) higher with propylene glycol, as compared to patch without enhancer. The maximum solubility of pioglitazone in Duro-Tak 87-2516 was found to be 6% w/w. Increasing the drug content in patch enhanced the transdermal flux and was highest when the pioglitazone level was 6% w/w (72.68 ± 5.76 µg/cm2/h). In vivo pharmacokinetic data demonstrate that the AUC0-α in transdermal application (13,506.51 ± 1649.92 ng·h/mL) was ~2 times higher (p < 0.0001) as compared to oral dosage form. In conclusion, the promising results observed here signifies that developed patch could be a viable alternative for oral therapy of pioglitazone.

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Section: Resultsmentioning

confidence: 99%

Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch

et al. 2019

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“…One concerning issue regarding TDS is that after usage and upon removal of the system there is still a significant portion of the drug remaining, which not only has an abuse potential-especially in case of opioids-but also as a safety concern for the patients, family members, caregivers, and the environment [17]. The FDA Guidance for Industry-Residual Drugs in Transdermal and Related Drug Delivery Systems [37]-addresses the issue of residual drug in TDS from a safety perspective.…”

Section: Discussionmentioning

confidence: 99%

“…It has been shown that the maximum skin penetration rate is depended on the thermodynamic activity (saturation state) rather than the concentration value [16]. Hence, in the majority of TDSs, the drug is loaded close to the saturation solubility in order to achieve a high thermodynamic activity and a greater force for passive diffusion across the skin [17,18] Increasing the drug loading to reach the saturation state in the TDS makes such systems unstable as there is a high probability of drug crystallization during storage [19][20][21]. Crystallization of the drug is a major challenge in the design and formulating of TDS as it makes the TDS unstable, reduces the amount of available drug, and decreases the intended flux [21,22].…”

Section: Introductionmentioning

confidence: 99%

Effect of Different Pressure-Sensitive Adhesives on Performance Parameters of Matrix-Type Transdermal Delivery Systems

Bozorg

Banga

2020

Pharmaceutics

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Matrix-type transdermal delivery systems (TDS) are comprised of the drug dissolved or dispersed in a pressure-sensitive adhesive (PSA) matrix and are designed to provide a controlled delivery through the skin and into systemic circulation. PSAs can directly affect the permeation, release, and performance characteristics of the system. In this study we aimed to design and characterize transdermal delivery systems formulated with lidocaine—as the model drug—loaded in different PSAs, including silicone, polyisobutylene (PIB), and acrylate. TDS containing lidocaine at its saturation points were prepared by the solvent casting method. In vitro permeation studies across dermatomed porcine ear skin were performed using Franz diffusion cells. In vitro release studies were carried out using USP apparatus 5 (paddle over disk). The cumulative amount permeated from the acrylate was significantly higher than silicone and PIB. The acrylate TDS contained a ten times higher drug amount than silicone TDS, but the permeation flux was only two folds higher. Results also showed the release of drug does not linearly correlate to saturation, as the silicone TDS comprising of the lowest amount of drug loading, showed the highest percentage release indicating the choice of PSA affected the drug release and permeation profile.

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“…The samples withdrawn were filtered and used for analysis. The amount of drug permeated was determined using HPLC analysis [40]. The cumulative drug release (CDR %) was estimated by the following expression:…”

Section: Ex Vivo Permeability Kineticsmentioning

confidence: 99%

In-Silico Validation and Fabrication of Matrix Diffusion-Based Polymeric Transdermal Patches for Repurposing Gabapentin Hydrochloride in Neuropathic Pain

Singh

Agarwal

Pancham

et al. 2021

CNSNDDT

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Background: Gabapentin (GBP) is an FDA approved drug for the treatment of partial and secondary generalized seizures, apart from being used for diabetic neuropathic pain. GBP displays highly intricate mechanism of action and its inhibitory response in elevated antagonism of NMDA (N-methyl-D-aspartate receptor) receptor and thus, can be repurposed for controlling neuropathic pain. Objective: Therefore, in the present study, we have selected hBCATc (human Pyridoxal 5’-phosphate dependent branched-chain aminotransferase cytosolic) gene that is highly expressed in neuropathic stressed conditions. Thereafter, have analyzed the GBP as its competitive inhibitor by homology modeling, molecular docking, also predicting its structural alerts and pharmacokinetic suitability through ADMET. However, GBP was found to be a potential drug in controlling neuropathic pain, still it has certain critical pharmacokinetics limitations therefore, the need for its targeted delivery was required and the same was attained by designing a GBP loaded trandermal patch (TDP). Methods: A suitable and equally efficacious GBP – TDP was developed by solvent evaporation method using PVP and HPMC in ratio of 2:1 as a polymer base for reservoir type of TDP. Also, PEG 400 was used as a plasticizer and PVA (4%) was taken for backing membrane preparation and then the optimized GBP-TDP was subjected for physical characterization, optimization and ex vivo release kinetics. Methods: A suitable and equally efficacious GBP – TDP was developed by solvent evaporation method using PVP and HPMC in ratio of 2:1 as a polymer base for reservoir type of TDP. Also, PEG 400 was used as a plasticizer and PVA (4%) was taken for backing membrane preparation and then the optimized GBP-TDP was subjected for physical characterization, optimization and ex vivo release kinetics. Results and conclusion: The results showed desired specifications with uneven and flaky surface appearance giving an avenue for controlled release of the drugs with 92.34 ± 1.43% of drug release in 10 h, further suggesting that GBP-TDP can be used as an effective tool against diabetic neuropathy pain.

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Formulation optimization of a drug in adhesive transdermal analgesic patch

Abstract: Drug-in-adhesive patches using CDB and APAP were developed for infants and children. Addition of OA enhanced solubility and permeation of drugs.

Cited by 12 publications

References 28 publications

Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch

Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch

Effect of Different Pressure-Sensitive Adhesives on Performance Parameters of Matrix-Type Transdermal Delivery Systems

In-Silico Validation and Fabrication of Matrix Diffusion-Based Polymeric Transdermal Patches for Repurposing Gabapentin Hydrochloride in Neuropathic Pain

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