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Eur J Pharm Sci. 2014 Dec 18;65:183-91. doi: 10.1016/j.ejps.2014.09.019. Epub 2014 Sep 28.

(Copper-curcumin) β-cyclodextrin vaginal gel: delivering a novel metal-herbal approach for the development of topical contraception prophylaxis.

Author information

1
DBT Lab, Indo-Soviet Friendship College of Pharmacy, Moga, Punjab, India.
2
Department of Virology, Haffkine Institute for Training Research and Testing, Parel, Mumbai, India.
3
DBT Lab, Indo-Soviet Friendship College of Pharmacy, Moga, Punjab, India. Electronic address: amitkumargoyal1979@gmail.com.

Abstract

Delivering a safe and effective topical vaginal contraceptive is the need of present era. We explored the potential of a metal (copper) and herbal moiety (curcumin) for this topical contraceptive prophylaxis. Complex of copper and curcumin (Cu-Cur) was synthesized and the concerns regarding its aqueous solubility was resolved by including it into the hydrophobic cavity of β-cyclodextrin (β-CD) as (Cu-Cur)CD inclusion complex. Dose assessment was made on the basis of in-vitro spermicidal assays and cell cytotoxicity studies. Finally the (Cu-Cur)CD loaded vaginal gel was prepared, characterized and evaluated for in-vitro spermicidal activity and preclinical toxicity studies. Spectral and morphological characterizations confirmed the synthesis of (Cu-Cur) and (Cu-Cur)CD inclusion complex. Spermicidal assays and Hela cell cytotoxic data revealed an optimized 1.5% (Cu-Cur)CD for further studies. 1.5% w/w (Cu-Cur)CD loaded carbopol 974p gel provided 100% motility even at 2-fold dilution and preclinical toxicity studies in Rats and Rabbits revealed its highly safe profile. The hypothesis of considering metal-herbal complex and its cyclodextrin complex has worked and the well planned strategy of including it in (β-CD) cavity provided a preeminent platform for vaginal delivery. In-vitro assays and preclinical toxicity analysis confirmed its potential to be used as highly safe and effective prophylaxis.

KEYWORDS:

Copper–curcumin; Nano-inclusion complex; Spermicidal gel; β-Cyclodextrin

PMID:
25266573
DOI:
10.1016/j.ejps.2014.09.019
[Indexed for MEDLINE]

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