Formulation Development of a Thermoresponsive Topical Gel of Cannabidiol for Dermatological Conditions

Authors' Affiliations

Akeemat Tijani, Adela Adu Agyemang, Alanis Vang, and Yareliz Pellot-Soto, Department of Pharmaceutical Sciences, East Tennessee State University, Johnson City, TN

Location

D.P. Culp Center Ballroom

Start Date

4-5-2024 9:00 AM

End Date

4-5-2024 11:30 AM

Poster Number

73

Name of Project's Faculty Sponsor

Dr. Ashana Puri

Faculty Sponsor's Department

Pharmaceutical Sciences

Classification of First Author

Clinical Doctoral Student

Competition Type

Competitive

Type

Poster Presentation

Presentation Category

Health

Abstract or Artist's Statement

Cannabidiol (CBD) has garnered considerable attention in research circles for its potential therapeutic benefits in managing various skin conditions, including acne, eczema, psoriasis, and skin cancer. Its promising medicinal properties extend to enhancing skin protection, bolstering barrier function, and expediting wound healing. Nevertheless, administering CBD poses challenges owing to its extremely lipophilic nature and limited skin permeation capabilities. This study investigates using a thermoresponsive topical CBD gel across microneedle-treated skin to enhance dermal delivery of CBD. A CBD solution was to be formulated that would gel at skin temperature hypothesizing that some solution would quickly permeate the skin through the microchannels and the gel would sustain the drug release and delivery over time, thus reducing the frequency of product application. An HPLC method was developed and validated adhering to the International Conference on Harmonization (ICH) guidelines for analytical assessment. The solubility of CBD was assessed across a range of solvents. Optimal formulations were developed by systematically testing varying percentages of excipients along with CBD and a thermoresponsive polymer. The optimal formulation was subjected to in vitro permeation testing on intact and microneedle-treated porcine ear skin using Franz diffusion cells for 72 h. The developed HPLC method involved isocratic elution on Kinetex® 5 µm 100 Ao, 250 X 4.6 mm C18 column, at a flow rate of 1 mL/min and column temperature of 25°C, after injecting 50 µL of sample and using acetonitrile: water (75:25) as mobile phase and UV detection at 212 nm. The linearity range was found to be between 0.1-50 µg/mL. Limits of drug detection and quantitation for samples in polyethylene glycol: 1X phosphate-buffered saline (1:1) were determined to be 0.03 and 0.08 µg/mL, respectively. No interference from the skin was observed at the drug’s retention time. CBD solubility was maximized in a combined solvent of propylene glycol, ethanol, and water. The optimal aqueous formulation contained 1% CBD, 10% propylene glycol, 25% ethanol, and 25% Pluronic and demonstrated an in vitro gelation time of 10 min on porcine skin. The change in viscosity from the solution (545 cp) to gel (1100 cp) was measured using a Brookfield viscometer. The amount of CBD in the epidermis and dermis was not found to be significantly different between intact and microneedle-treated skin after 72 h (p>0.05), depicting higher CBD binding to the skin due to its lipophilicity, negating the effect of microchannels on its delivery. Future studies will focus on investigating the effect of skin microporation on the rate of CBD delivery into the skin layers and designing suitable CBD-loaded microneedles for deeper and targeted penetration into the dermis for effective treatment of dermatological conditions.

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Apr 5th, 9:00 AM Apr 5th, 11:30 AM

Formulation Development of a Thermoresponsive Topical Gel of Cannabidiol for Dermatological Conditions

D.P. Culp Center Ballroom

Cannabidiol (CBD) has garnered considerable attention in research circles for its potential therapeutic benefits in managing various skin conditions, including acne, eczema, psoriasis, and skin cancer. Its promising medicinal properties extend to enhancing skin protection, bolstering barrier function, and expediting wound healing. Nevertheless, administering CBD poses challenges owing to its extremely lipophilic nature and limited skin permeation capabilities. This study investigates using a thermoresponsive topical CBD gel across microneedle-treated skin to enhance dermal delivery of CBD. A CBD solution was to be formulated that would gel at skin temperature hypothesizing that some solution would quickly permeate the skin through the microchannels and the gel would sustain the drug release and delivery over time, thus reducing the frequency of product application. An HPLC method was developed and validated adhering to the International Conference on Harmonization (ICH) guidelines for analytical assessment. The solubility of CBD was assessed across a range of solvents. Optimal formulations were developed by systematically testing varying percentages of excipients along with CBD and a thermoresponsive polymer. The optimal formulation was subjected to in vitro permeation testing on intact and microneedle-treated porcine ear skin using Franz diffusion cells for 72 h. The developed HPLC method involved isocratic elution on Kinetex® 5 µm 100 Ao, 250 X 4.6 mm C18 column, at a flow rate of 1 mL/min and column temperature of 25°C, after injecting 50 µL of sample and using acetonitrile: water (75:25) as mobile phase and UV detection at 212 nm. The linearity range was found to be between 0.1-50 µg/mL. Limits of drug detection and quantitation for samples in polyethylene glycol: 1X phosphate-buffered saline (1:1) were determined to be 0.03 and 0.08 µg/mL, respectively. No interference from the skin was observed at the drug’s retention time. CBD solubility was maximized in a combined solvent of propylene glycol, ethanol, and water. The optimal aqueous formulation contained 1% CBD, 10% propylene glycol, 25% ethanol, and 25% Pluronic and demonstrated an in vitro gelation time of 10 min on porcine skin. The change in viscosity from the solution (545 cp) to gel (1100 cp) was measured using a Brookfield viscometer. The amount of CBD in the epidermis and dermis was not found to be significantly different between intact and microneedle-treated skin after 72 h (p>0.05), depicting higher CBD binding to the skin due to its lipophilicity, negating the effect of microchannels on its delivery. Future studies will focus on investigating the effect of skin microporation on the rate of CBD delivery into the skin layers and designing suitable CBD-loaded microneedles for deeper and targeted penetration into the dermis for effective treatment of dermatological conditions.