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Nanoparticulate System for the Transdermal Delivery of Catechin as an Antihypercholesterol: In Vitro and In Vivo Evaluations.

ABSTRACT: Gambir (Uncaria gambir, Roxb.) contains catechins that is often empirically used to treat various diseases. Catechins can reduce cholesterol levels by inhibiting coenzyme HMG-CoA reductase that plays a role in cholesterol metabolism. Research has been carried out covering the optimization of transethosomal catechins, the formulation of Transethosomal Catechin Gel (TCG) and Non-Transethosomal Catechin Gel (NTCG), which were then tested for catechin permeation from these gel preparations in vitro using Franz's diffusion cell with PTFE membranes. The anti-hypercholesterol activity test was carried out with Simvastatin orally as a positive control using 25 male Wistar rats (Rattus norvegicus). The catechin transetosomes have a size of 176.1 ± 5.8 nm, Zeta potential -11.6 ± 5.28, and Entrapment Efficacy of 96.77% ± 0.05. The result of cumulative catechins that permeated from TCG and NTCG were and 172.454 ± 5.287 and 112.741 ± 2.241 μg respectively. Permeation test graphs showed similar permeation and flux profiles. TCG can reduce total cholesterol and LDL (Low Density Lipoprotein) values in rats by 39.77% and 51.52% respectively during 14 days of use.

SUBMITTER: Mita SR

PROVIDER: S-EPMC9505170 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature

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Nanoparticulate System for the Transdermal Delivery of Catechin as an Antihypercholesterol: In Vitro and In Vivo Evaluations.

Mita Soraya Ratnawulan SR Abdassah Marline M Supratman Unang U Shiono Yoshihito Y Rahayu Driyanti D Sopyan Iyan I Wilar Gofarana G

Pharmaceuticals (Basel, Switzerland) 20220913 9

Gambir (<i>Uncaria gambir</i>, Roxb.) contains catechins that is often empirically used to treat various diseases. Catechins can reduce cholesterol levels by inhibiting coenzyme HMG-CoA reductase that plays a role in cholesterol metabolism. Research has been carried out covering the optimization of transethosomal catechins, the formulation of Transethosomal Catechin Gel (TCG) and Non-Transethosomal Catechin Gel (NTCG), which were then tested for catechin permeation from these gel preparations in ...[more]

PMID: 36145363

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Project description:BackgroundPhloretin (Phl) is a flavonoid compound that contains multiple phenolic hydroxyl groups. It is found in many plants, such as apple leaves, lychee pericarp, and begonia, and has various biological activities, such as antioxidant and anticancer effects. The strong hydrogen bonding between Phl molecules results in poor water solubility and low bioavailability, and thus the scope of the clinical application of Phl is limited. Therefore, it is particularly important to improve the water solubility of Phl for its use to further combat or alleviate skin aging and oxidative damage and develop antioxidant products for the skin. The purpose of this study was to develop and evaluate a phloretin transfersome gel (PTG) preparation for transdermal drug delivery to improve the bioavailability of the drug and delay aging.MethodsPhloretin transfersomes (Phl-TFs) were prepared and optimized by the thin-film dispersion-ultrasonication method. Phl-TFs were characterized by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD). The Log P method was used to determine the solubility of the Phl-TFs. The skin penetration ability of the prepared PTG was evaluated using the Franz diffusion cell method. In addition, the in vivo pharmacokinetics of PTG were studied in rats, and an antioxidant activity investigation was conducted using a D-gal rat model.ResultsPhl-TFs were successfully prepared with a Soybean Phosphatidylcholine (SPC)/CHOL ratio of 2.7:1 w/v, a phloretin concentration of 1.3 mg/mL, a hydration time of 46 min, an ultrasound time of 5 min, and an ultrasound power of 180 W. The Log P was 2.26, which was significantly higher than that of phloretin (p < 0.05, paired t test). The results of the in vitro penetration test demonstrated that the cumulative skin penetration of the Phl-TFs after 24 h was 842.73 ± 20.86 μg/cm2. The data from an in vivo pharmacokinetic study showed that the Cmax and AUC of PTG were 1.39- and 1.97-fold higher than those of the phloretin solution gel (PSG), respectively (p < 0.05, paired t test). The experimental results in aging rats showed that PTG had a better antioxidant effect.ConclusionsPhl-TFs and PTG preparations with a good shape, safety, and stability were successfully prepared. In vivo pharmacokinetics and preliminary antioxidant experiments further verified the transdermal penetration and antioxidant activity of the phloretin transdermal drug delivery preparation, providing an experimental basis for its further development.

Dataset Information

Nanoparticulate System for the Transdermal Delivery of Catechin as an Antihypercholesterol: In Vitro and In Vivo Evaluations.

Publications

Nanoparticulate System for the Transdermal Delivery of Catechin as an Antihypercholesterol: In Vitro and In Vivo Evaluations.

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