Development and characterization of floating spheroids of atorvastatin calcium loaded NLC for enhancement of oral bioavailability

Sharma, Kritika; Hallan, Supandeep Singh; Lal, Bharat; Bhardwaj, Ankur; Mishra, Neeraj

doi:10.3109/21691401.2015.1041637

Cited by 21 publications

(13 citation statements)

References 19 publications

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“…The correlation coefficient (R 2 ) for each model was calculated. Model giving R 2 nearer to 1 was selected as the best fit model for the drug release [29,30].…”

Section: Release Kineticsmentioning

confidence: 99%

Development and optimization of sulforaphane-loaded nanostructured lipid carriers by the Box-Behnken design for improved oral efficacy against cancer: in vitro, ex vivo and in vivo assessments

Soni

Rizwanullah

Kohli

2017

Artificial Cells, Nanomedicine, and Biotechnology

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In the present study, sulforaphane (SFN)-loaded nanostructured lipid carriers (NLC) were developed and optimized for improved oral efficacy against cancer. The SFN-loaded NLC formulation was developed by melt emulsification ultrasonication technique and optimized by Box-Behnken statistical design. The optimized SFN-loaded NLC formulation composed of precirol ATO 5 (solid lipid) and vitamin E (liquid lipid) as lipid phase (3% w/v), poloxamer 188 (1%) and Tween 80 (1%) as surfactant. The mean particle size, polydispersity index, zeta potential, entrapment efficiency (%) and drug loading (%) of optimized SFN-loaded NLC formulation was observed to be 145.38 ± 4.46 nm, 0.181 ± 0.023, -25.12 ± 2.36 mV, 84.94 ± 3.82% and 14.82 ± 3.46%, respectively. In vitro drug release studies showed that the release of SFN from optimized NLC formulation was significantly higher (86.52 ± 5.48%) compared to SFN suspension (38.47 ± 5.52%) up to 24 h. Ex vivo gut permeation studies revealed a very good enhancement in permeation of drug present in the NLC compared to plain SFN solution and were further confirmed by CLSM. MTT assay in different cancer cell lines showed that the optimized SFN-loaded NLC formulation exhibited significantly improved (p < .05) cytotoxicity compared to free SFN solution. SFN-loaded NLC formulation showed significantly improved antioxidant activity compared to free SFN solution. Furthermore, pharmacokinetic study on albino Wistar rats showed 5.04-fold increase in relative oral bioavailability with NLC (p < .05) compared to SFN suspension. Therefore, NLC represents a great potential for improved efficacy of SFN after oral administration.

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“…The correlation coefficient (R 2 ) for each model was calculated. Model giving R 2 nearer to 1 was selected as the best fit model for the drug release [29,30].…”

Section: Release Kineticsmentioning

confidence: 99%

Development and optimization of sulforaphane-loaded nanostructured lipid carriers by the Box-Behnken design for improved oral efficacy against cancer: in vitro, ex vivo and in vivo assessments

Soni

Rizwanullah

Kohli

2017

Artificial Cells, Nanomedicine, and Biotechnology

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“…Rod‐shaped extrudates were subsequently broken into spherical particles. Finally, the spherical particles or spheroids were dried at room temperature (Bataille et al, 1998; Jacob et al, 1998; Sharma et al., 2016).…”

Section: Methodsmentioning

confidence: 99%

“…Pellips refers to the sphericity of the spheroids. Pellips was calculated with 50 LPS (Sharma et al., 2016).

Pellips = \frac{p}{π \times d max}

…”

Section: Methodsmentioning

confidence: 99%

“…The drum was rotated at 25 rpm for 4 min and the fines were removed by passing through a sieve of 250 mm mesh size. The fraction above 250 mm mesh (Ma) was used to calculate the friability of LPS (Kilor et al., 2010; Sharma et al., 2016).

Friablity (% F) = \frac{M b - M a}{italicMb} \times 100 .

…”

Section: Methodsmentioning

confidence: 99%

“…As a result, in many cases, the required therapeutic level of PHF may not be achieved (Kesarwani, Gupta, & Mukerjee, 2013; Manach et al., 2004). To overcome these limitations, a suitable novel drug delivery system is required which has high therapeutic efficacy and enhanced bioavailability (Bataille, Iderne, Jacob, & Jacob, 1998; Jacob, Bataille, Jacob, & Iderne, 1998; Sharma, Hallan, Lal, Bhardwaj, & Mishra, 2016).…”

Section: Introductionmentioning

confidence: 99%

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Development and characterization of spheroidal antidiabetic polyherbal formulation from fresh vegetable juice: A novel approach

et al. 2020

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Polyherbal Formulations (PHF) were developed by combining fruit juices of Momordica charantia, Cucumis sativus, and Solanum lycopersicum in different ratios and optimized through Oral Glucose Tolerance Test (OGTT) model. PHF-C pretreated rats showed the highest reduction of Serum Glucose Levels (SGL) after 60 min of glucose administration. PHF-C was incorporated into spheroids using fresh juice (FJS) and lyophilized powder (LPS) of selected plants. In OGTT study, LPS showed a significant reduction of SGL. LPS was characterized as almost spherical, having disintegration time 8 min, adequate friability, and good flow properties. In STZ-induced diabetic rats on 7th, 14th, and 21st days, LPS was reduced SGL by 9.01%, 20.9%, 38.9% (250 mg/ kg dose); 20.5%, 33.9%, and 50.7% (500 mg/kg dose), respectively. LPS showed a significant improvement in abnormal body weight, biochemical, and oxidative parameters in comparison to PHF-C and metformin. Novel formulation LPS (500 mg/ kg) was found more effective (p < .05) in reversing STZ-induced hyperglycemia as compared to PHF-C (1,000 mg/kg) and at par with metformin (500 mg/kg). Practical applications Fresh vegetable juice contains large quantities of vitamins and minerals. Cooking and processing of fruits may destroy their nutritional value. However, FJS also has some limitations, including seasonal specificity, patient compliance, less stability, loss of vitamins and fibers, abnormal sugar level, weak immunity, and difficult to carry by patients. Lyophilization is a well-known method to improve the physical state, shelf life, and stability of phytoconstituents. Poor absorption and less bioavailability also impede the acceptance of PHF. To overcome these limitations, a suitable novel drug delivery system is required which has high therapeutic efficacy and enhanced bioavailability. The patented spheroids of herbal extracts which are in use for the treatment of the number of diseases encouraged the present work. Spheroid protects the constituents of herbal drugs from gastric destruction and gut bacteria. The outcome of present research supports the concept of enhanced stability and bioavailability of phytoconstituents present in FJS.

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Genetic Algorithm with Model-Updating-Based PLS Regression for the Spectrophotometric Determination of Clopidogrel, Atorvastatin, and Aspirin in the Presence of its Degradation Product

et al. 2020

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Development and characterization of floating spheroids of atorvastatin calcium loaded NLC for enhancement of oral bioavailability

Cited by 21 publications

References 19 publications

Development and optimization of sulforaphane-loaded nanostructured lipid carriers by the Box-Behnken design for improved oral efficacy against cancer: in vitro, ex vivo and in vivo assessments

Development and optimization of sulforaphane-loaded nanostructured lipid carriers by the Box-Behnken design for improved oral efficacy against cancer: in vitro, ex vivo and in vivo assessments

Development and characterization of spheroidal antidiabetic polyherbal formulation from fresh vegetable juice: A novel approach

Genetic Algorithm with Model-Updating-Based PLS Regression for the Spectrophotometric Determination of Clopidogrel, Atorvastatin, and Aspirin in the Presence of its Degradation Product

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