Enhanced and reliable BA will help in establishing its therapeutic usefulness especially for neurodegenerative and cancerous disorders in humans.

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Background: Envisaging the poor solubility (56ng/ml) and permeability of tetrahydrocurcumin (THCC), it was formulated into lipidic nanostructures to enhance its bioavailability upon topical application to promote the healing process for skin inflammatory disorders. Lack of literature on suitable method for determining THCC per se and nanoformulations prompted us to develop a RP-HPLC method to detect the drug in its nanostructures and in pig ear skin post dermatokinetics. Objective: The present investigation aimed to develop a simple, precise and RP-HPLC method for the quantitative estimation of THCC in prepared lipidic nanostructures, its ointment and in skin homogenate obtained post dermatokinetic study. Method: THCC encapsulated nanostructures and ointment were formulated using modified emulsification method and embedded into an ointment base to enhance its spreadability and improve patient compliance. A fast and sensitive reverse phase high performance liquid chromatography method was developed using a Hypersil BDS reverse phase C18 column (4.6 mm × 250 mm, 5 μm) with mobile phase comprising tetrahydrofuran (THF) and 1 mgmL-1 citric acid (4:6), at a flow rate of 1.0 mLmin−1 with a run time of 20 min. Result: THCC nanostructures were successfully prepared using spontaneous microemulsification method. THCC was detected at 282 nm and revealed two peaks which were attributed to the keto-enol tautomerism in the molecule with retention times of 6.23 min and 11.06 min respectively. The assay of THCC in nanostructures and ointment was found to be 98.30% and 99.98% with entrapment efficiency 77.00±2.74 %. The dermatokinetic studies revealed sufficient release of THCC from its ointment up till 24 hr with a concentration of 1382 μgcm-2, for causing a therapeutic effect. Conclusion: The method was found to be reproducible and robust as shown by low coefficient of variation and a constant analyte/IS ratio. It was successfully employed for the estimation of THCC assay in nanostructures and it’s ointment and dermatokinetic analysis in skin.

Background:: All-trans retinoic acid (ATRA) is widely employed in the treatment of various proliferative and inflammatory diseases. However, its therapeutic efficacy is imperiled due to its poor solubility and stability. Latter was surmounted by its incorporation into a solid matrix of lipidic nanoparticles (SLNs). Methods:: ATRA loaded SLNs (ATRA-SLNs) were prepared using novel microemulsification technique (USPTO 9907758) and an optimal composition and were characterized in terms of morphology, differential scanning calorimetry (DSC) and powder X-ray diffraction studies (PXRD). In vitro release, oral plasma pharmacokinetics (in rats) and stability studies were also done. Results:: Rod-shaped ATRA-SLNs could successfully incorporate 3.7 mg/mL of ATRA, increasing its solubility (from 4.7μg/mL) by 787 times, having an average particle size of 131.30 ± 5.0 nm and polydispersibility of 0.283. PXRD, DSC, and FTIR studies confirmed formation of SLNs. Assay/total drug content and entrapment efficiency of ATRA-SLNs was 92.50± 2.10% and 84.60±3.20% (n=6), respectively, which was maintained even on storage for one year under refrigerated conditions as aqueous dispersion. In vitro release in 0.01 M phosphate buffer (pH 7.4) with 3% tween 80 was extended 12 times from 2h for free ATRA to 24 h for ATRA-SLNs depicting Korsmeyer Peppas release. Oral administration in rats showed 35.03 times enhanced bioavailability for ATRA-SLNs. Conclusion:: Present work reports preparation and evaluation of bioenhanced ATRA-SLNs containing high concentration of ATRA (> 15 times than that reported by others). Latter is attributed to novel preparation process and intelligent selection of components.