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Summary
Ocular esterase activity varies between albino and pigmented rabbits, with higher activity in pigmented rabbits
Area of Science:
- Pharmacology
- Ocular Biochemistry
- Drug Delivery
Background:
- Prodrug design requires understanding in vivo enzymatic conditions for drug regeneration.
- Ocular tissues (cornea, iris, ciliary body, aqueous humor) are critical for topical drug disposition.
Purpose of the Study:
- To characterize esterase activities in rabbit ocular tissues.
- To compare esterase activity between albino and pigmented rabbits.
- To inform the design and evaluation of ocular ester prodrugs.
Main Methods:
- Assessed hydrolysis kinetics of alpha-naphthyl acetate.
- Used aqueous humor and homogenates of cornea, iris, and ciliary body.
- Incubated samples with and without esterase inhibitors.
Main Results:
- Esterase activity was highest in iris-ciliary body, followed by cornea, then aqueous humor.
- Multiple esterases likely present in ocular tissues and fluids.
- Pigmented rabbits showed greater esterase activity in cornea and iris-ciliary body than albino rabbits.
Conclusions:
- Ocular esterase activity influences the hydrolysis of ester-containing drugs and prodrugs.
- Differences in esterase activity between rabbit breeds necessitate using both for prodrug evaluation.
- This research aids in rational prodrug design for improved ocular drug efficacy.