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

Abstract

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.

Pioglitazone, a Peroxisome Proliferator-Activated Receptor-γ Agonist, Downregulates the Inflammatory Response in Cutaneous Leishmaniasis Patients Without Interfering in Leishmania braziliensis Killing by Monocytes

“…Regarding the effects observed during the use of pioglitazone, it has been mainly reported that it increases insulin sensitivity, interference with lipid homeostasis, and regulation of the inflammatory response. Thus, many efforts have been made in the development of formulations for the topical use of pioglitazone ( Silva-Abreu et al., 2017 ; Nair et al., 2019 ; Rojewska et al., 2020 ), opening new expectations for the treatment of skin diseases such as CL. Indeed, patients with psoriasis treated with topical pioglitazone had a decreased severity in disease score ( Mittal et al., 2009 ; Singh and Anil, 2016 ).…”

Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation

“…The micrograph of the film was captured on a Nova NanoSEM 450 (FEI Ltd., Hillsboro, OR, USA) equipped with a large field detector. The film was mounted using silver electrical tape and sputter coated (SCD005 Baltek Sputter Coater, Baltec, AG, Balzers, Liechtenstein, Germany) with gold in the presence of argon gas under reduced pressure [ 32 ].…”

Transdermal Patches for the Treatment of Angina Pectoris: An Effective Drug Delivery System-a Review

“…This patch gained the largest share of the nitroglycerin industry. Nitro-Dur II ® was the brand name for the patch, which was later sold and listed in a US patent [77].…”