The authors prepared surface modified (with polyelectrolyte layers), tea polyphenols (TPP) encapsulated, gelatin nanoparticles (TPP-GNP) and characterised them. The size of the spherical nanoparticles was-50 nm. Number of polyelectrolyte layers and incubation time influenced the encapsulation efficiency (EE); highest EE was noted in nanoparticles with six polyelectrolyte layers (TPP-GNP-6L) incubated for 4 h. TPP released from TPP-GNP-6L in simulated biological fluids indicated protection and controlled release of TPP due to encapsulation. Mathematical modelling indicated anomalous type as a predominant mode of TPP release. TPP-GNP-6L exhibited enhanced pharmacokinetics in rabbit model compared with free TPP. The area under the concentration-time curve and mean residence time were significantly higher in TPP-GNP-6L compared with free TPP which provide an evidence of higher bioavailability of TPP due to encapsulation. The authors demonstrated that encapsulation of TPP into GNPs favoured slow and sustained release of TPP with improved pharmacokinetics and bioavailability thereby can prolong the action of TPP. © The Institution of Engineering and Technology 2016.

Abul Kalam Azad Mandal

Department of Biotechnology

School of Bio Sciences and Technology

Vellore Campus

Kulandaivelu K

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

IET Nanobiotechnology

Epigallocatechin-3-gallate (EGCG), derived from green tea, is an active phytochemical against many types of cancer, cardiovascular, neurological and inflammatory diseases. However, its pharmaceutical activity is limited due to low bioavailability and chemical instability. To overcome these limitations, we fabricated spherical, EGCG loaded solid lipid nanoparticles (SLN-EGCG) as an oral delivery system. The SLN-EGCG showed a hydrodynamic diameter of 300.2 ± 3.8 nm with the drug encapsulation efficiency of 81 ± 1.4%. Additionally, a slow and sustained release of EGCG was noted. Mathematical modeling of release kinetic data suggested that the SLN-EGCG followed the Higuchi model and released EGCG via fickian diffusion method. The data on pharmacokinetic parameters indicated significantly improved bioavailability and protection of EGCG from degradation due to encapsulation into SLN. The SLN-EGCG did not show any acute or sub-chronic toxicity when compared with free EGCG in the rat model. Together these data supported the hypothesis that SLN-EGCG is capable of enhancing the bioavailability and stability of EGCG and can be used as an alternative system for oral administration of EGCG. © 2019, © 2019 Informa UK Limited, trading as Taylor &amp; Francis Group.

Drug Development and Industrial Pharmacy

Pharmacokinetic, toxicokinetic, and bioavailability studies of epigallocatechin-3-gallate loaded solid lipid nanoparticle in rat model

In the present study, we fabricated epigallocatechin-3-gallate (EGCG) loaded albumin nanoparticles (Alb-NP-EGCG) to enhance bioavailability and improve pharmacokinetic parameters of EGCG. The physicochemical properties of the Alb-NP-EGCG were studied using scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and in vitro release studies. Characterization of Alb-NP-EGCG indicated the formation of spherical nanoparticles with no drug and excipient interaction. Alb-NP-EGCG showed a high drug loading capacity of 92%. Further, in vitro study showed a sustained release of EGCG from Alb-NP-EGCG over a period of 48 h. Mathematical modeling and release kinetics indicated that the Alb-NP-EGCG followed zero order kinetic and EGCG was released via fickian diffusion method. In vivo bioavailability and distribution of Alb-NP-EGCG showed an enhanced plasma concentration of EGCG with 1.5 fold increase along with prolonged T1/2 of 15.6 h in the system when compared with the free EGCG. All this study demonstrated the fabrication of EGCG loaded albumin nanoparticles which favored the slow and sustained release of EGCG with improved pharmacokinetics and bioavailability thereby prolonging the action of EGCG. Additional acute and sub-acute toxicity test of the Alb-NP-EGCG demonstrated the safety of the Alb-NP-EGCG. Therefore, the Alb-NP-EGCG could be a promising drug delivery system for EGCG. © 2019, King Abdulaziz City for Science and Technology.

Fulltext

3 Biotech

Encapsulation of epigallocatechin-3-gallate into albumin nanoparticles improves pharmacokinetic and bioavailability in rat model

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Improved bioavailability and pharmacokinetics of tea polyphenols by encapsulation into gelatin nanoparticles

Journal	IET Nanobiotechnology
Publisher	Institution of Engineering and Technology (IET)
ISSN	1751-8741
Open Access	0