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Evaluation of epithelial transport and oxidative stress protection of nanoengineered curcumin derivative-cyclodextrin formulation for ocular delivery

Archives of Pharmacal Research 2019년 42권 10호 p.909 ~ 925
 ( Maharjan Pooja ) - Inje University College of Pharmacy

 ( Jin Min-Ki ) - Inje University College of Pharmacy
 ( Kim Da-Seul ) - Inje University College of Pharmacy
 ( Yang Jae-Wook ) - Inje University College of Medicine Department of Ophthalmology
 ( Maharjan Anjila ) - Inje University College of Pharmacy
 ( Shin Meong-Cheol ) - Gyeongsang National University College of Pharmacy
 ( Cho Kwan-Hyung ) - Inje University College of Pharmacy
 ( Kim Man-Su ) - Inje University College of Pharmacy
 ( Min Kyoung-Ah ) - Inje University College of Pharmacy


Ocular drug delivery has been a well-known route for the drug administration for the treatment of ocular diseases. However, numerous anatomical and physiological barriers prevailing in the eye itself create considerable challenges for achieving the necessitated therapeutic efficacy along with ocular bioavailability. However, recent advances in nanoengineered strategies hold definite promises in terms of devising improved ophthalmic medicines for the effective drug delivery to target the sites with enhanced ocular bioavailability. Curcumin, a hydrophobic polyphenol yellow colored compound, and its metabolic reduced product, tetrahydrocurcumin (THC), have been known for their beneficial pharmacological functions, such as anti-inflammatory or anti-oxidant activities at various tissue sites. However, the low aqueous solubility of these compounds results in their poor bioavailability, thereby limiting their widespread application. Therefore, in the present study, we investigated the changes in drug solubility by forming inclusion complexes with different derivatives of hydroxypropyl (HP)-cyclodextrins (CD). To this end, the spray drying technique was used for nanoengineering curcumin or THC-loaded formulations to improve the stability of formulations during the storage. The formulations were characterized in terms of physicochemical properties and cellular permeability. The results demonstrated that the encapsulation of curcumin (or THC) into the HP-CDs significantly increased the drug solubility and enhanced the corneal and retinal epithelial permeability. Curcumin or THC complexes in HP-CDs with improved bioavailability also induced anti-oxidant activity (SOD1, CAT1, and HMOX1) in higher levels in the ocular epithelial cells and showed oxidative protection effects in rabbit cornea tissues that will boost up their application in ocular medicine.


Ophthalmic formulation; Curcumin; Tetrahydrocurcumin; Cyclodextrins; Cellular transport; Human corneal epithelium; Retinal pigmented epithelium
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