TY - JOUR

T1 - Orcinol Glucoside Loaded Polymer - Lipid Hybrid Nanostructured Lipid Carriers: Potential Cytotoxic Agents against Gastric, Colon and Hepatoma Carcinoma Cell Lines

AU - Nahak, Prasant

AU - Gajbhiye, Rahul L.

AU - Karmakar, Gourab

AU - Guha, Pritam

AU - Roy, Biplab

AU - Besra, Shila Elizabeth

AU - Быков, Алексей Геннадьевич

AU - Акентьев, Александр Владимирович

AU - Носков, Борис Анатольевич

AU - Nag, Kaushik

AU - Jaisankar, Parasuraman

AU - Panda, Amiya Kumar

N1 - Funding Information: Financial support in the form of research grant (SR/S1/PC/ 32/2011, INT/RUS/RFBR/P-220) from the Department of Science and Technology, Govt. of India, and Russian Foundation of Basic Research (RFBR № 15–53-45043_IND_a) are sincerely acknowledged. P.N. and R.G. acknowledge the receipt of research fellowships from the UGC, New Delhi [P.N.: RGNF for disabled, No. F./2012– 13/RGNF-2012-13D-GENCHH-51106/31-Oct-2013; R.G: Grant no F. 14–2(SC)/2010 (SA-III)].

PY - 2018/10/1

Y1 - 2018/10/1

N2 - Purpose: Orcinol glucoside (OG) - loaded nanostructured lipid carrier (NLC), coated with polyethylene glycol-25/55-stearate (PEG-25/55-SA), were explored for delivering OG to improve in vitro cytotoxicity against gastrointestinal tract (GIT), colon and hepatoma carcinoma cell lines. It is being expected that the PEGylated formulations would possess the sustainability in withstanding the adverse physiological extremities like the most significant metabolic activities and phase I / II enzymatic activities in the intestines. Methods: NLCs were prepared using tristearin, oleic acid and PEG-25/55-stearate by hot homogenization-ultrasonic dispersion; characterized by DLS, TEM, SEM, AFM, entrapment efficiency and drug loading capacity studies. Results: NLC diameter ranged from 160 to 230 nm with negative zeta potential of −8 to −20 mV. TEM/SEM and AFM studies suggest spherical and smooth surface morphologies. Differential scanning calorimetry studies reveal the loss of crystallinity when OG was incorporated into the NLC. NLCs showed initial burst release, followed by sustained release of OG. PEG-NLC exhibited superior anticancer activity against GIT and also in hepatoma cancer cell lines. Conclusions: This is the first report demonstrating a practical approach for possible oral delivery of OG in GIT and targeting hepatoma cancer, warranting further in vivo studies for superior management of GIT cancer.

AB - Purpose: Orcinol glucoside (OG) - loaded nanostructured lipid carrier (NLC), coated with polyethylene glycol-25/55-stearate (PEG-25/55-SA), were explored for delivering OG to improve in vitro cytotoxicity against gastrointestinal tract (GIT), colon and hepatoma carcinoma cell lines. It is being expected that the PEGylated formulations would possess the sustainability in withstanding the adverse physiological extremities like the most significant metabolic activities and phase I / II enzymatic activities in the intestines. Methods: NLCs were prepared using tristearin, oleic acid and PEG-25/55-stearate by hot homogenization-ultrasonic dispersion; characterized by DLS, TEM, SEM, AFM, entrapment efficiency and drug loading capacity studies. Results: NLC diameter ranged from 160 to 230 nm with negative zeta potential of −8 to −20 mV. TEM/SEM and AFM studies suggest spherical and smooth surface morphologies. Differential scanning calorimetry studies reveal the loss of crystallinity when OG was incorporated into the NLC. NLCs showed initial burst release, followed by sustained release of OG. PEG-NLC exhibited superior anticancer activity against GIT and also in hepatoma cancer cell lines. Conclusions: This is the first report demonstrating a practical approach for possible oral delivery of OG in GIT and targeting hepatoma cancer, warranting further in vivo studies for superior management of GIT cancer.

KW - cancer . cytotoxic activity . GIT . hepatoma . NLC .OG . PEG

KW - GIT

KW - PEG

KW - NLC

KW - hepatoma

KW - OG

KW - cancer

KW - cytotoxic activity

UR - http://www.scopus.com/inward/record.url?scp=85052317537&partnerID=8YFLogxK

U2 - 10.1007/s11095-018-2469-3

DO - 10.1007/s11095-018-2469-3

M3 - Article

VL - 35

SP - 1

EP - 10

JO - Pharmaceutical Research

JF - Pharmaceutical Research

SN - 0724-8741

IS - 10

M1 - 198

ER -