Synthesis of PLGA nanoparticles of tea polyphenols and their strong in vivo protective effect against chemically induced DNA damage.

作者: Yogeshwer Shukla , Srivastava , Bhatnagar , Singh , Mishra

DOI: 10.2147/IJN.S26364

关键词: DNAIn vivoXRCC1DNA repairPharmacologyDMBABioavailabilityMaterials scienceDNA damageBiochemistryTheaflavin

摘要: In spite of proficient results several phytochemicals in preclinical settings, the conversion rate from bench to bedside is not very encouraging. Many reasons are attributed this limited success, including inefficient systemic delivery and bioavailability under vivo conditions. To achieve improved efficacy, polyphenolic constituents black (theaflavin [TF]) green (epigallocatechin-3-gallate [EGCG]) tea poly(lactide-co-glycolide) nanoparticles (PLGA-NPs) were entrapped with entrapment efficacy ~18% 26%, respectively. Further, their preventive potential against 7,12-dimethylbenzanthracene (DMBA)-induced DNA damage mouse skin using alkaline unwinding assay was evaluated. Pretreatment (topically) either TF or EGCG (100 μg/mouse) doses exhibits protection 45.34% 28.32%, respectively, DMBA-induced damage. However, pretreatment TF-loaded PLGA-NPs protects 64.41% by 1/20th dose bulk, 71.79% 1/10th 72.46% 1/5th bulk. Similarly, 51.28% (1/20th bulk), 57.63% (1/10th 63.14% (1/5th bulk) prevention noted EGCG-loaded PLGA-NP doses. These showed that polyphenol-loaded have ~30-fold dose-advantage than bulk Additionally, TF- significant for induction repair genes (XRCC1, XRCC3, ERCC3) suppression responsive (p53, p21, MDM2, GADD45α, COX-2) as compared respective Taken together, a superior ability prevent at much lower concentrations, thus opening new dimension chemoprevention research.

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