Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies

被引：46

作者：

Rathore, Charul ^{[1
]}

Hemrajani, Chetna ^{[2
]}

Sharma, Abhishek Kumar ^{[2
]}

Gupta, Piyush Kumar ^{[3
]}

Jha, Niraj Kumar ^{[4
]}

Aljabali, Alaa A. A. ^{[5
]}

Gupta, Gaurav ^{[6
]}

Singh, Sachin Kumar ^{[7
]}

Yang, Jen-Chang ^{[8
]}

Dwivedi, Ram Prakash ^{[9
]}

Dua, Kamal ^{[10
]}

Chellappan, Dinesh Kumar ^{[11
]}

Negi, Poonam ^{[12
]}

Tambuwala, Murtaza M. ^{[12
,13
]}

机构：

[1] Chandigarh Univ, Univ Inst Pharma Sci, Ajitgarh, Punjab, India

[2] Shoolini Univ Biotechnol & Management Sci, Sch Pharmaceut Sci, Solan 173212, India

[3] Sharda Univ, Sch Basic Sci & Res SBSR, Dept Life Sci, Knowledge Pk 3, Greater Noida 201310, Uttar Pradesh, India

[4] Sharda Univ, Sch Engn & Technol SET, Dept Biotechnol, Greater Noida 201310, Uttar Pradesh, India

[5] Yarmouk Univ, Fac Pharm, Dept Pharmaceut & Pharmaceut Technol, Irbid 21163, Jordan

[6] Suresh Gyan Vihar Univ, Sch Pharm, Jaipur 302017, Rajasthan, India

[7] Lovely Profess Univ, Sch Pharmaceut Sci, Phagwara, Punjab, India

[8] Taipei Med Univ, Coll Biomed Engn, Grad Inst Nanomed & Med Engn, Taipei 11052, Taiwan

[9] Shoolini Univ, Sch Elect & Comp Sci Engn, Solan, HP, India

[10] Univ Technol Sydney, Grad Sch Hlth, Discipline Pharm, Ultimo, NSW 2007, Australia

[11] Int Med Univ, Sch Pharm, Dept Life Sci, Kuala Lumpur 57000, Malaysia

[12] Ulster Univ, Sch Pharm & Pharmaceut Sci, Coleraine BT52 1SA, County Londonde, North Ireland

[13] Univ Lincoln, Lincoln Sch Med, Brayford Pool Campus, Lincoln LN6 7TS, England

来源：

DRUG DELIVERY AND TRANSLATIONAL RESEARCH | 2023年 / 13卷 / 01期

关键词：

SNEDDS; Thermodynamic stability; Bioavailability; Hepato-toxicity; In vitro release kinetics; IN-VITRO; ENHANCED BIOAVAILABILITY; FORMULATION DEVELOPMENT; DISSOLUTION RATE; DESIGN; ABSORPTION; POLYSACCHARIDE; NANOCARRIERS; PERMEABILITY; LIDOCAINE;

D O I：

10.1007/s13346-022-01193-8

中图分类号：

TH7 [仪器、仪表];

学科分类号：

0804 ; 080401 ; 081102 ;

摘要：

Thymoquinone (TQ) is an antioxidant, anti-inflammatory, and hepatoprotective compound obtained from the black seed oil of Nigella sativa. However, high hydrophobicity, instability at higher pH levels, photosensitivity, and low oral bioavailability hinder its delivery to the target tissues. A self-nanoemulsifying drug delivery system (SNEDDS) was fabricated using the microemulsification technique to address these issues. Its physicochemical properties, thermodynamic stability studies, drug release kinetics, in vivo pharmacokinetics, and hepatoprotective activity were evaluated. The droplet size was in the nano-range (< 90 nm). Zeta potential was measured to be -11.35 mV, signifying the high stability of the oil droplets. In vivo pharmacokinetic evaluation showed a fourfold increase in the bioavailability of TQ-SNEDDS over pure TQ. Furthermore, in a PCM-induced animal model, TQ-SNEDDS demonstrated significant (p<0.05) hepatoprotective activity compared to pure TQ and silymarin. Reduction in liver biomarker enzymes and histopathological examinations of liver sections further supported the results. In this study, SNEDDS was demonstrated to be an improved oral delivery method for TQ, since it potentiates hepatotoxicity and enhances bioavailability.

引用

页码：292 / 307

页数：16

共 66 条

[1]

AbuKhader M.M., 2017, J BIONANOSCIENCE, V11, P258, DOI [10.1166/jbns.2017.1447, DOI 10.1166/JBNS.2017.1447]

[2] Albumin Nano-Encapsulation of Piceatannol Enhances Its Anticancer Potential in Colon Cancer Via Downregulation of Nuclear p65 and HIF-1α [J].