Abstract
Resveratrol and oxyresveratrol are natural polyphenolic stilbenes with several important pharmacological activities. However, low solubility and aqueous instability are the major limitations in their drug delivery applications. In the present work, we demonstrated the encapsulation of resveratrol and oxyresveratrol with nanosponge to improve solubility and stability. Several characterization techniques were used to confirm the encapsulation of both drug molecules within the nanosponges. The high encapsulation efficiency of resveratrol (77.73%) and oxyresveratrol (80.33%) was achieved within the nanosponges. Transmission electron microscopy suggested uniform spherical size particles of resveratrol and oxyresveratrol loaded nanosponges. Compared to free drugs, better protection against UV degradation was observed for resveratrol-loaded nanosponge (2-fold) and oxyresveratrol-loaded nanosponge (3-fold). Moreover, a higher solubilization of resveratrol- and oxyresveratrol-loaded nanosponges lead to a better antioxidant activity compared to drug molecules alone. Cytotoxicity studies against DU-145 prostate cancer cell lines further suggested improved activity of both resveratrol and oxyresveratrol-loaded nanosponges without any significant toxicity of blank nanosponges.
Highlights
Both resveratrol and oxyresveratrol are naturally occurring polyphenolic stilbenes obtained from a variety of plant sources [1]
We illustrated the synthesis cyclodextrin nanosponges the encapsulation of RES
We illustrated the synthesis of cyclodextrin nanosponges and the encapsulation of RES and OXY
Summary
Both resveratrol (trans-3,40 ,5-trihydroxystilbene; RES, Figure 1a) and oxyresveratrol (trans-20 ,3,40 , 5-tetrahydroxystilbene, OXY, Figure 1b) are naturally occurring polyphenolic stilbenes obtained from a variety of plant sources [1]. OXY was isolated naturally from mulberry (Morus Alba L.) and Artocarpus lakoocha Roxburgh (Moraceae) in abundance [4,5]. Pharmaceutics 2019, 11, 545; doi:10.3390/pharmaceutics11100545 www.mdpi.com/journal/pharmaceutics activity against herpes simplex virus [9,10,11]. Both drugs exhibit several challenges in drug delivery as RES and OXY are chemically unstable molecules because of their photosensitivity and undergo oxidative degradation in aqueous solution.
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