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Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Dermal and transdermal delivery: prodrugs
Kenneth B Sloan1, Hemamalini Devarajan-Ketha, Scott C Wasdo
1Department of Medicinal Chemistry, University of Florida, PO Box 100485, Gainesville, Fl 32610, USA. sloan@cop.ufl.edu
Therapeutic Delivery
|July 27, 2012
Summary
Optimizing drug physicochemical properties with prodrugs enhances dermal and transdermal delivery. Evaluating prodrugs at saturation is crucial for accurate assessment of optimal skin penetration.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Dermatology
Background:
- Dermal and transdermal drug delivery face challenges due to suboptimal drug physicochemical properties.
- The stratum corneum presents a significant barrier to drug permeation.
- Prodrug strategies can transiently modify drug properties to improve skin penetration.
Purpose of the Study:
- To investigate the role of prodrugs in optimizing drug physicochemical properties for enhanced skin delivery.
- To determine the critical parameters for designing effective prodrugs for dermal and transdermal applications.
- To emphasize the importance of evaluating prodrugs under saturated conditions.
Main Methods:
- Prodrug design to modulate drug lipophilicity and aqueous solubility.
- Evaluation of prodrugs in saturated solutions to maximize thermodynamic activity.
- Assessment of drug and prodrug partitioning and permeation across the stratum corneum.
Main Results:
- Prodrugs can be engineered to possess improved lipid and aqueous solubilities, facilitating stratum corneum traversal.
- Evaluation at sub-saturation concentrations can lead to erroneous conclusions regarding prodrug efficacy.
- Optimal prodrug design requires balancing both lipophilic and hydrophilic characteristics.
Conclusions:
- Prodrugs are a viable strategy to overcome physicochemical limitations for dermal and transdermal drug delivery.
- Thermodynamic activity, assessed via saturated solutions, is a key determinant of prodrug performance.
- Successful prodrug development necessitates optimizing both solubility parameters for effective skin permeation.
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