Overcoming the dissolution rate, gastrointestinal permeability and oral bioavailability of glimepiride and simvastatin co-delivered in the form of nanosuspension and solid self-nanoemulsifying drug delivery system: A comparative study

Pandey, Narendra Kumar; Singh, Sachin Kumar; Gulati, Monica; Kumar, Bimlesh; Kapoor, Bhupinder; Ghosh, Dipanjoy; Kumar, Rajan; Khursheed, Rubiya; Awasthi, Ankit; Kuppusamy, Gowthamarajan; Wadhwa, Sheetu; Satija, Saurabh; Dureja, Harish; Jain, Subheet Kumar; Chellappan, Dinesh Kumar; Anand, Krishnan; Mehta, Meenu; Dua, Kamal

doi:10.1016/j.jddst.2020.102083

Cited by 26 publications

(12 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The results clearly indicated that the nanosuspension containing both the drugs have shown better recovery of cells as compared to their SNEDDS formulations. This could be due to better permeability, Cmax and AUC of drugs loaded in nanosuspension with respect to SNEDDS as reported in previous investigation (Pandey et al 2020).…”

Section: Histopathological Studiessupporting

confidence: 68%

“…About 6.69-and 4.22-folds increase in the area under the curves (AUCs) of GLM present in nanosuspensions and SNEDDS and about 1.76-and 2.68-folds increase AUCs of SIM present in nanosuspensions and SNEDDS were reported as compared to their unprocessed forms. Interestingly, the results indicated that the AUCs of nanosuspensions of GLM and SIM were 1.59 and 1.52 higher than SNEDDS respectively (Pandey et al 2020). These positive outcomes of aforementioned studies helped to initiate the pharmacodynamic studies for the formulations on high fat diet and streptozotocin induced rat model.…”

Section: Resultsmentioning

confidence: 98%

“…The formulation development, its characterization and pharmacokinetic studies have been reported in the recent publication (Pandey et al 2020). It was observed that the particle size of SP-NS was found to be 127.4±1.…”

Section: Resultsmentioning

confidence: 99%

See 2 more Smart Citations

Expanding arsenal against diabetes mellitus through nanoformulations loaded with glimepiride and simvastatin: A comparative study

Pandey

Singh

Kumar

et al. 2022

Environ Sci Pollut Res

Self Cite

View full text Add to dashboard Cite

Type 2 diabetes mellitus is one of the most common and life-threatening diseases found across the globe. It occurs due to insulin resistance (IR). Major causes of IR include obesity, sedentary life style and hyperlipidemia. Glimepiride (GLM) is one of the most common oral sulphonyl ureas that is being used to treat diabetes and Simvastatin (SIM) is one of the most common statins that is used to treat hyperlipidaemia. However, both the drugs suffer from dissolution rate limited oral bioavailability. In the present study two such drugs, GLM and SIM were co-formulated into nanosuspension (NS) as well as self-nanoemulsifying drug delivery systems (L-SNEDDS). Both formulations were spray dried for solidi cation and evaluated for their antidiabetic potential against high fat diet and streptozotocin induced rat model. The study showed signi cant (p< 0.05) decrease in lipid/cholesterol and blood glucose levels and signi cant increase in antioxidant levels in the rats treated with NS and SNEDDS containing the drugs alone as well as their combination as compared to their unprocessed forms.However, the e cacy was more prominent in case of combination possibly due to dual bene ts i.e., decrease in IR due to statin and control of blood glucose level. Among NS and SNEDDS, NS was found more e cacious than that of the SNEDDS possibly due to higher enhancement of oral bioavailability in case of NS.

show abstract

Section: Histopathological Studiessupporting

confidence: 68%

Section: Resultsmentioning

confidence: 98%

See 1 more Smart Citation

Expanding arsenal against diabetes mellitus through nanoformulations loaded with glimepiride and simvastatin: A comparative study

Pandey

Singh

Kumar

et al. 2022

Environ Sci Pollut Res

Self Cite

View full text Add to dashboard Cite

show abstract

“…SEDDS are comprised of a mixture of surfactants, oils, and solvents, with the ability to re-arrange within an aqueous environment to improve oral absorption. However, the commercial application of this technology is still limited because the efficiency of oral absorption of SEDDS drugs is dependent on factors such as oil to surfactant ratio, surfactant concentration, the polarity of the emulsion, and the size and charge of droplets (Singh et al, 2017;Ghosh et al, 2020;Khursheed et al, 2020;Pandey et al, 2020;Kumar et al, 2021).…”

Section: Introductionmentioning

confidence: 99%

A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum

et al. 2021

View full text Add to dashboard Cite

Albendazolum (ABZ) is a BCS class II drug. It has challenging biopharmaceutical properties, which include poor solubility and dissolution rate. These properties have laid the ground for developing a supersaturated self-nanoemulsifying drug delivery system (S-SNEDDS) to form oil-in-water nanoemulsion in situ to improve the oral bioavailability of ABZ. Based on the ABZ solubility, emulsifying ability, and stability after dispersion in an aqueous phase, an optimal self-nanoemulsifying drug delivery system (SNEDDS) consisting of oleic acid, Tween ® 20, and PEG 600 (X:Y:Z, w/w) was identified, having 10% (w/w) hydroxypropyl methylcellulose (HPMC) E15 lv as its precipitation inhibitor. The optimized system possessed a small mean globule size value (89.2 nm), good dispersion properties (polydispersity index (PDI): 0.278), and preserved the supersaturated state of ABZ. S-SNEDDS was transformed into solid supersaturated self-nanoemulsifying drug delivery systems (SS-SNEDDS) using microcrystalline cellulose as a solid material. The developed S-SNEDDS were characterized for globule size, pH, turbidity, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and flow properties. The data obtained from the results suggest that this S-SNEDDS formulation can enhance the solubility and oral bioavailability of ABZ for appropriate clinical application.

show abstract

“…The physicochemical characteristics of SN and DN suggest that they are suitable for self-nanoemulsifying drug delivery system (SNEDDS) as such system is reported to improve drug solubility, permeability, and bioavailability after oral administration (Kazi et al., 2017 ; Pandey et al., 2020 ). Liquid SNEDDS can be easily filled into soft/hard gelatin capsules and converted into solid dosage form in a single step process via spray drying, adsorption techniques.…”

Section: Introductionmentioning

confidence: 99%

Development and optimization of sitagliptin and dapagliflozin loaded oral self-nanoemulsifying formulation against type 2 diabetes mellitus

et al. 2020

View full text Add to dashboard Cite

Control of hyperglycemia and prevention of glucose reabsorption (glucotoxicity) are important objectives in the management of type 2 diabetes. This study deals with an oral combined dosage form design for two anti-diabetic drugs, sitagliptin and dapagliflozin using self-nanoemulsifying drug delivery systems (SNEDDS). The SNEDDS were developed using naturally obtained bioactive medium-chain/long-chain triglycerides oil, mixed glycerides and nonionic surfactants, and droplet size was measured followed by the test for antioxidant activities. Equilibrium solubility and dynamic dispersion experiments were conducted to achieve the maximum drug loading. The in vitro digestion, in vivo bioavailability, and anti-diabetic effects were studied to compare the representative SNEDDS with marketed product Dapazin ® . The representative SNEDDS containing black seed oil showed excellent self-emulsification performance with transparent appearance. Characterization of the SNEDDS showed nanodroplets of around 50–66.57 nm in size (confirmed by TEM analysis), in addition to the high drug loading capacity without causing any precipitation in the gastro-intestinal tract. The SNEDDS provided higher antioxidant activity compared to the pure drugs. The in vivo pharmacokinetic parameters of SNEDDS showed significant increase in C max (1.99 ± 0.21 µg mL −1 ), AUC (17.94 ± 1.25 µg mL −1 ), and oral absorption (2-fold) of dapagliflozin compared to the commercial product in the rat model. The anti-diabetic studies showed the significant inhibition of glucose level in treated diabetic mice by SNEDDS combined dose compared to the single drug therapy. The combined dose of sitagliptin-dapagliflozin using SNEDDS could be a potential oral pharmaceutical product for the improved treatment of type 2 diabetes mellitus.

show abstract

Overcoming the dissolution rate, gastrointestinal permeability and oral bioavailability of glimepiride and simvastatin co-delivered in the form of nanosuspension and solid self-nanoemulsifying drug delivery system: A comparative study

Cited by 26 publications

References 35 publications

Expanding arsenal against diabetes mellitus through nanoformulations loaded with glimepiride and simvastatin: A comparative study

Expanding arsenal against diabetes mellitus through nanoformulations loaded with glimepiride and simvastatin: A comparative study

A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum

Development and optimization of sitagliptin and dapagliflozin loaded oral self-nanoemulsifying formulation against type 2 diabetes mellitus

Contact Info

Product

Resources

About