Abstract
Background: Yellow curcumin, the “Indian Gold” is known since ancient times to modulate the activities of a wide variety of targets. The voluminous literature and several patents are a proof of the therapeutic value of curcumin. Tetrahydrocurcumin (THC), however, has remained as an unexplored molecule although its cosmeceutical properties have been documented. Their compromised bioavailability, poor aqueous solubility (curcumin 11 ng/mL, THC 56ng/mL), high log P (Cur: 3.28; THC: 2.98) are hurdles for developing as potential drugs. Objective: This article discusses the usefulness of lipidic nanoparticles of curcumin and THC for skin inflammation. Method: Nanocouturing to produce lipidic nanoparticles (LNs) of curcumin and THC was done via an optimized microemulsification technique. LNs were characterized by FTIR, TEM, pharmacokinetics, and pharmacodynamic study. Results: FTIR reflected the suitable incorporation of drugs into LNs. TEM examination revealed a spherical to ellipsoidal shape with a particle size of <200 nm. In vitro release study indicates the release of both drugs is between 70-80% within 24 h. Ex-vivo permeation studies confirmed the ability of LNs to cross the stratum corneum. Stability studies (Q1AR2) indicated that both were stable, safe, and nonirritating (OECD 404). Xylene induced ear edema model of inflammation showed both molecules to possess equivalent abilities to treat inflammation. Conclusion: Curcumin being yellow in color is unstable at physiological pH and plasma and possesses poor bioavailability, while THC is a colorless stable molecule, making it a molecule of choice to be developed as an effective topical product.
Published Version
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