Formulation of Topical Delivery Using Vardenafil for the Management of Symptoms Related to Raynaud’s Phenomenon
Abstract
Raynaud’s phenomenon is a disorder of thermoregulation causing excessive vasoconstriction, especially in the fingers during cold exposure. Attacks typically progress from ischemia to cyanosis to erythema, and severe cases may lead to ulcers or gangrene. Currently, no FDA approved treatments exist for Raynaud’s Phenomenon, but providers may treat with various off-label prescriptions. One class of drugs used are type-5 phosphodiesterase inhibitors (PDE5i), but these drugs can come with adverse effects. These effects, like hypotension, could be minimized in a topical delivery formulation that is not reliant on full systemic absorption. Vardenafil is an appropriate candidate for this approach because it possesses physicochemical properties favorable for skin permeation. The drug was quantified using high-performance liquid chromatography (HPLC) with potassium phosphate buffer (0.070 M, pH 4.5) and acetonitrile (70:30) as the mobile phase and Phenomenex Kinetex C18 column (5 µm, 250 × 4.6 mm). To assess the permeation of drug across the skin with the Franz cell set up, an appropriate receptor solution needs to be identified. Solubility studies were therefore conducted using varying concentrations of polyethylene glycol-40 (PEG-40) and transcutol individually prepared in phosphate buffered saline (PBS, 3:2, 1:1, 2:3, 3:7, 2:8, 1:9), as well as varying concentrations of Volpo 20 in PBS (0.1-6% w/v). Transcutol exhibited the highest solubility in 60% Transcutol (4.66 ± 0.31 mg/mL). PEG-40 demonstrated a saturation concentration of 1.06 ± 0.05 mg/mL at 60%, while Volpo-20 achieved 0.77 ± 0.02 mg/mL at 6%. [PA1.1][AS1.2]Based on these findings, 60% Transcutol was initially selected as the medium; however, during method validation, the high viscosity of the solvent interfered with the instrument’s performance. As PEG-40 exhibited even greater viscosity, 6% Volpo-20 was ultimately selected as the receptor solution due to improved analytical compatibility. Ongoing studies involve optimizing and validating the HPLC method for the selected solvent.
Start Time
15-4-2026 9:00 AM
End Time
15-4-2026 12:00 PM
Room Number
Culp Ballroom 316
Poster Number
7
Presentation Type
Poster
Presentation Subtype
Posters - Competitive
Presentation Category
Science, Technology, and Engineering
Student Type
Graduate and Professional Degree Students, Residents, Fellows
Faculty Mentor
Ashana Puri
Formulation of Topical Delivery Using Vardenafil for the Management of Symptoms Related to Raynaud’s Phenomenon
Culp Ballroom 316
Raynaud’s phenomenon is a disorder of thermoregulation causing excessive vasoconstriction, especially in the fingers during cold exposure. Attacks typically progress from ischemia to cyanosis to erythema, and severe cases may lead to ulcers or gangrene. Currently, no FDA approved treatments exist for Raynaud’s Phenomenon, but providers may treat with various off-label prescriptions. One class of drugs used are type-5 phosphodiesterase inhibitors (PDE5i), but these drugs can come with adverse effects. These effects, like hypotension, could be minimized in a topical delivery formulation that is not reliant on full systemic absorption. Vardenafil is an appropriate candidate for this approach because it possesses physicochemical properties favorable for skin permeation. The drug was quantified using high-performance liquid chromatography (HPLC) with potassium phosphate buffer (0.070 M, pH 4.5) and acetonitrile (70:30) as the mobile phase and Phenomenex Kinetex C18 column (5 µm, 250 × 4.6 mm). To assess the permeation of drug across the skin with the Franz cell set up, an appropriate receptor solution needs to be identified. Solubility studies were therefore conducted using varying concentrations of polyethylene glycol-40 (PEG-40) and transcutol individually prepared in phosphate buffered saline (PBS, 3:2, 1:1, 2:3, 3:7, 2:8, 1:9), as well as varying concentrations of Volpo 20 in PBS (0.1-6% w/v). Transcutol exhibited the highest solubility in 60% Transcutol (4.66 ± 0.31 mg/mL). PEG-40 demonstrated a saturation concentration of 1.06 ± 0.05 mg/mL at 60%, while Volpo-20 achieved 0.77 ± 0.02 mg/mL at 6%. [PA1.1][AS1.2]Based on these findings, 60% Transcutol was initially selected as the medium; however, during method validation, the high viscosity of the solvent interfered with the instrument’s performance. As PEG-40 exhibited even greater viscosity, 6% Volpo-20 was ultimately selected as the receptor solution due to improved analytical compatibility. Ongoing studies involve optimizing and validating the HPLC method for the selected solvent.
