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

Rathore, Charul; Hemrajani, Chetna; Sharma, Abhishek Kumar; Gupta, Piyush Kumar; Jha, Niraj Kumar; Aljabali, Alaa A. A.; Gupta, Gaurav; Singh, Sachin Kumar; Yang, Jen‐Chang; Dwivedi, Ram Prakash; Dua, Kamal; Chellappan, Dinesh Kumar; Negi, Poonam; Tambuwala, Murtaza M.

doi:10.1007/s13346-022-01193-8

Cited by 28 publications

(14 citation statements)

References 66 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Zeta potential was found to be −11.35 mV, indicating the high stability of the oil droplets. Pharmacokinetic assessment in rats revealed a fourfold increase in the bioavailability of the TQ-self-nanoemulsifying drug delivery system over pure TQ [ 69 ]. Similarly, the relative bioavailability of TQ was enhanced 3.87-fold by a self-nanoemulsifying drug delivery system in comparison with TQ suspension [ 70 ].…”

Section: Resultsmentioning

confidence: 99%

Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review

Mahomoodally

Aumeeruddy²,

Legoabe³

et al. 2022

IJMS

View full text Add to dashboard Cite

Despite existing conventional hypoglycemic drugs to manage diabetes, their non-availability and cost in low-income countries coupled with the associated side effects remain a major concern. Consequently, exploring for alternative treatments to manage diabetes has been a continuous priority. Nigella sativa L. (NS) (Family: Ranunculaceae) is regarded as a valuable traditional remedy in diabetes management and extensively studied for its biological properties. This systematic review provides a comprehensive and critical analysis of clinical studies on the efficacy, safety, and mechanism of action of NS and its compound thymoquinone (TQ) in diabetes management. The main scientific databases which were scrutinised were Scopus, PubMed, Google Scholar, and Web of Science. Data search was conducted from inception to January 2022. A total of 17 clinical studies were obtained; 16 studies on Nigella sativa L. and 1 study on its compound TQ. N. sativa was found to be highly potent in terms of its hypoglycemic activity when compared to placebo based on improvement in parameters including fasting blood glucose (FBG), postprandial blood glucose (PPBG), Hemoglobin A1C (HbA1c), homeostatic model assessment for insulin resistance (HOMA-IR), and homeostatic model assessment for assessment of beta-cell functionality (HOMA-β). The compound TQ in combination with a daily dose of metformin demonstrated a greater reduction in the levels of HbA1c and blood glucose compared to metformin alone. The bioavailability of TQ can be enhanced by using nanoparticulate drug delivery systems. Considering the findings of the clinical studies along with negligible adverse effects, NS has strong potential application in bioproduct development for the management of diabetes. Further investigations should explore the detailed mechanism of actions by which TQ exerts its therapeutic antidiabetic effects to provide more insights into its clinical use in the management of diabetes.

show abstract

Section: Resultsmentioning

confidence: 99%

Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review

Mahomoodally

Aumeeruddy²,

Legoabe³

et al. 2022

IJMS

View full text Add to dashboard Cite

show abstract

“…Storage of the diluted self emulsions at room temperature for 8 hours allowed for the detection of phase separation and drug precipitation. 13…”

Section: Formulation Of Sneddsmentioning

confidence: 99%

“…Thus, the region of the figure where the Smix concentration is greatest is also known as a nanoemulsion or a monophasic region. 13…”

Section: Pseudo Ternary Diagram Of Exmmentioning

confidence: 99%

“…Self Emulsification Time The phase separation of the spontaneously emulsifying system is highly sensitive to the dilution and pH of the vehicle. 13 Because of this, certain EXM SNEDDS were diluted twice (20 times) and thrice (100 times) using different solvents (i.e. water, 0.1 N HCl and phosphate buffer).…”

Section: Optical Claritymentioning

confidence: 99%

“…This occurs because SNEDDS is a preconcentrate combination that contains surfactants, cosurfactants, and a lipophilic phase. 12,13 The EXM SNEDDS were made utilising the water titration approach, and the ultrasonication technique will be used to further reduce their size. Develop formulation was characterized for dilution study, optical clarity, emulsification time, drug content, viscosity, size, PDI, and stability studies.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Formulation and evaluation of self-nanoemulsifying drug delivery system for improved oral delivery of exemestane hydrochloride

Prajapati

Prajapati²,

Khunt³

2023

IJCAAP

View full text Add to dashboard Cite

Exemestane HCl (EXM) is a new irreversible steroidal aromatase inhibitor for adjuvant therapy of hormonally sensitive breast cancer in post-menopausal women. EXM's low water solubility hinders solid oral dosage form development. The current work aims to increase EXM solubility by formulating the self nanoemulsifying drug delivery (SNEDDs) system. The water titration approach was employed in the development of SNEDDs. Based on solubility tests, SNEDDs components Caprol Microexpress and Labrafac were selected as oil phase, Tween 80 as surfactant, and Triacetin as co-surfactant. Phase investigations were carried out with various surfactant:co-surfactant ratios (1:1, 1:2, 1:3, 2:1, 3:1). Tween 80: triacetin (1:2) and (1:3) with Caprol Microexpress and Labrafac alone had the greatest nanoemulsion area. Visual evaluation, optical clarity, particle size, medication concentration, and viscosity were used to optimise 10 formulations. F3, F7, and F8 batches had the lowest size at 7.313 ± 1.44 nm, 6.379 ± 0.45 nm, and 14.67 ± 0.37 nm, respectively, with self-emulsification times under 1 min.But optical clarity data was suggested that F7 was not showing any precipitation up to 24 H. Overall, the developed SNEDDS formulation could be a promising approach for the improved oral delivery of EXE with enhanced dissolution and bioavailability.

show abstract

Silk Meshes Coated with Chitosan‐Bioactive Phytochemicals Activate Wound Healing Genes In Vitro

Bokhari

Yasmeen

Ali

et al. 2023

Macromolecular Bioscience

View full text Add to dashboard Cite

Meshes from natural silk are hand knitted and surface functionalized to facilitate hernia repair and other load bearing, tissue applications. Purified organic silk is ‐ hand knitted and then coated with chitosan (CH)/bacterial cellulose (BC) blend polymer using four phytochemicals such as pomegranate (PG) peel, Nigella sativa (NS) seed, Licorice root (LE), and Bearberry leaf extracts (BE) separately. Characterizations using GCMS analysis shows the presence of bioactive chemicals in the extracts. Scanning electron microcopy (SEM) shows that the surface is coated with the composite polymer t. Fourier transform infrared spectroscopy (FTIR) shows significant elements found in CH, BC, and phytochemicals in plant extracts with no chemical changes. Tensile strength of the coated meshes is higher to support tissue as implants. The release kinetics suggest sustained release of phytochemical extracts. In vitro studies confirmed the noncytotoxic, biocompatible, wound healing potential of the meshes. Furthermore, gene expression analysis of 3‐wound healing genes shows marked increase in the in vitro cell cultures due to the presence of extracts. These results suggest that the composite meshes can efficiently support hernia closure while facilitating wound/tissue healing and combating bacterial infections. Therefore, these meshes can be good candidates for fistula and cleft palate repair.

show abstract

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

Cited by 28 publications

References 66 publications

Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review

Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review

Formulation and evaluation of self-nanoemulsifying drug delivery system for improved oral delivery of exemestane hydrochloride

Silk Meshes Coated with Chitosan‐Bioactive Phytochemicals Activate Wound Healing Genes In Vitro

Contact Info

Product

Resources

About