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Updated: Jul 16, 2026

Ocular Therapeutic Delivery and Advanced Tissue Retrieval in Adult Rats
Published on: May 23, 2025
Delivery of retinoid-based therapies to target tissues
Alexander R Moise1, Noa Noy, Krzysztof Palczewski
1Department of Pharmacology, School of Medicine, Case Western Reserve University, Cleveland, Ohio 44106-4965, USA. ram50@case.edu
Abstract:
Through its various metabolites, vitamin A controls essential physiological functions. Both naturally occurring metabolites and novel retinoid analogues have shown effectiveness in many clinical settings that include skin diseases and cancer, and in animal models of human conditions affecting vision. In this review, we analyze several potential retinoid-based therapies from the point of view of drug metabolism and transport to target tissues. We focus on the endogenous factors that affect the absorption, transport, and metabolism of retinoids by taking into account data obtained from the analysis of animal models that lack the enzymes or proteins involved in the storage and absorption of retinoids. We also discuss findings of toxicity associated with retinoids in an effort to improve the outcome of retinoid-based therapies. In this context, we review evidence that esterification of retinol and retinol-based drugs within target tissues provides one of the most efficient means to improve the absorption and to reduce the toxicity associated with pharmacological doses of retinoids. Future retinoid-based therapeutic strategies could involve targeted delivery mechanisms leading to lower toxicity and improved effectiveness of retinoids.
Insights
Vitamin A metabolites, known as retinoids, are crucial for physiological functions. Esterification of retinoids enhances absorption and reduces toxicity, improving therapeutic outcomes.
Area of Science:
- Biochemistry
- Pharmacology
- Physiology
Background:
- Vitamin A metabolites, or retinoids, are vital for numerous physiological functions.
- Retinoids demonstrate efficacy in treating skin diseases, cancer, and vision-related conditions.
Purpose of the Study:
- To review retinoid-based therapies focusing on drug metabolism and transport.
- To investigate endogenous factors influencing retinoid absorption, transport, and metabolism.
- To discuss retinoid toxicity and strategies for improving therapeutic outcomes.
Main Methods:
- Analysis of data from animal models lacking key retinoid absorption and storage proteins.
- Review of clinical and preclinical studies on retinoid metabolism and transport.
- Examination of esterification as a mechanism to enhance retinoid efficacy and safety.
Main Results:
- Endogenous factors significantly impact retinoid absorption, transport, and metabolism.
- Retinoid esterification within target tissues improves absorption and reduces toxicity.
- Targeted delivery systems show promise for future retinoid therapies.
Conclusions:
- Understanding retinoid metabolism and transport is key to optimizing therapies.
- Esterification is a promising strategy to enhance the safety and efficacy of retinoid drugs.
- Future research should focus on targeted delivery for improved retinoid-based treatments.
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