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Treatment of pulmonary arterial hypertension by vardenafil-solid dispersion lozenges as a potential alternative drug delivery system
Faculty
Pharmacy
Year:
2020
Type of Publication:
ZU Hosted
Pages:
Authors:
Azza Ali Hassan Solyman
Staff Zu Site
Abstract In Staff Site
Journal:
Journal of Drug Delivery Science and technology Elsevier
Volume:
Keywords :
Treatment , pulmonary arterial hypertension , vardenafil-solid dispersion lozenges
Abstract:
Pulmonary Arterial Hypertension (PAH) is a condition of increased blood pressure within the arteries of the lung. Vardenafil (VDF) is commonly used for alleviating pulmonary blood pressure but unfortunately; VDF has low bioavailability due to poor solubility and extensive first-pass metabolism after ordinary oral administration. Therefore, in this study, solid dispersion (SD) of VDF was prepared to enhance VDF dissolution rate and then incorporated into lozenges as a buccal dosage form for systemic drug delivery avoiding first-pass effect. Vardenafil solid dispersion (VDF-SD) lozenges (L1 formula) was selected as master formula due to its high release rate. Organ bio-distribution of VDF (20 mg/kg) following VDF-SD lozenges (L1) administration in adult albino female rats was investigated, and showed a significant increase in Cmax (≈11.55 times) and AUC0–4 h (≈11.81 times) of VDF in lung compared to oral administration of VDF suspension (p < 0.0001). In addition, cyclic guanosine monophosphate (cGMP) serum level, used as indicator of VDF in-vivo efficacy, was higher following VDF-SD lozenges (L1) administration, compared to that following oral administration of VDF suspension. This study suggests that administration of VDF as lozenges in the mouth cavity to be a potential alternative to oral route with superior therapeutic effect targeting pulmonary arterial hypertension.
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Azza Ali Hassan Solyman, "Formulation and Evaluation of Timolol Maleate Loaded Liposomes as an Ocular Drug Delivery System", Bull.Fac.Pharrm.Cairo Univ, 2005
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Department Related Publications
Ahmed Samer Zedan, "Controlled release of Diclofenac sodium from matrix tablet formulations.", لايوجد, 1900
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Ahmed Samer Zedan, "Process Analytical Technology: Nondestructive Evaluation of Cyclosporine A and Phospholipid Solid Dispersions by Near Infrared Spectroscopy and Chemical Imaging", لايوجد, 1900
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Azza Ali Hassan Solyman, "Design and in vitro characterization of small unilamellar niosomes as ophthalmic carrier of dorzolamide hydrochloride", Informa health, 2014
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Azza Ali Hassan Solyman, "Formulation and Evaluation of Timolol Maleate Loaded Niosomes as an Ocular Drug Delivery System", Bull.Fac.Pham.Cairo Univ., 2004
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Amr Selim Ahmed Ali Abu Lila, "Generation, characterization and in vivo biological activity of two distinct monoclonal anti-PEG IgMs", Elsevier, 2014
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