Mucoadhesive Microspheres of Atorvastatin Calcium: Rational Design, Evaluation and Enhancement of Bioavailability

Dewangan, Hitesh Kumar; Sharma, Aruna; Mishra, Ankit; Singour, Pradeep Kumar

doi:10.5530/ijper.55.3s.180

Cited by 21 publications

(8 citation statements)

References 16 publications

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“…Typically, the CQAs are termed the result of a product, which will represent its quality. In the current formulation development, PS, EE [14] and the drug release rate constant of the TCMs were selected as the responses R1, R2, and R3, respectively, and the same will be focused attentively during the entire development.…”

Section: Cqasmentioning

confidence: 99%

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

PRAGALLAPATI,

LAKSHMI PONNURI,

MURTHY KOLLAPALLI

2023

Int J App Pharm

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Objective: To develop floating microspheres for the topotecan in order to prevent its onversion into inactive carboxylate form in intestinal pH conditions so as to improve its bioavailability. Methods: Chitosan-based porous floating microspheres containing sodium bicarbonate by coacervation technique were developed. Quality by design approach using Box-Behnken Design was adopted to assess the influences of selected formulation variables and their importance on the quality of the finished product. Results: The selected model was analyzed and optimized. The microspheres floated immediately without any lag time upon addition into water and remained floatable for more than 24 h-1. The optimized formulation was found to have the particle size of 379.2 µm, entrapment efficiency of 76.3% and the drug release rate constant of 0.29 h i.e., the release was extended up to 16 h-1. Conclusion: The results affirmed that controlled-release porous microspheres of Topotecan with inherent floating without lag were successfully developed.

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Section: Cqasmentioning

confidence: 99%

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

PRAGALLAPATI,

LAKSHMI PONNURI,

MURTHY KOLLAPALLI

2023

Int J App Pharm

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“…The degree of swelling was then calculated by the following formula 𝐷𝑒𝑔𝑟𝑒𝑒 𝑜𝑓 𝑆𝑤𝑒𝑙𝑙𝑖𝑛𝑔 = (𝑀0 − 𝑀𝑡) 𝑀0) * 100 ⁄ Where, S.I = swelling index, M0 = weight of microsphere at the end and Mt = weight of microsphere at start. 16 Mucoadhesive property of microspheres was determined by in-vitro adhesion test. Eggshell membrane was used for this purpose.…”

Section: In-vitro Releasementioning

confidence: 99%

Formulation and evaluation of mucoadhesive microspheres of simvastatin using a 23 full factorial approach

Chandrabhan Gautam, Bharat Tyagi

2023

tjjpt

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The objective of the current investigation was to optimize and formulate mucoadhesive microspheres loaded with simvastatin utilizing guar gum as the mucoadhesive polymer and stabilizing the particles with magnesium stearate so that the formulation could control the release of the drug thereby reducing its dosing frequency and improving the bioavailability. The microspheres were prepared using emulsion coacervation method and the micromeritic features were evaluated. The yield of all the batches of microspheres was found to be reasonably good ranging from 52.96 % to 75.48 %. The drug loading was found to be 70.46 ± 0.130 to 74.63 ± 0.535 % while the size of microspheres ranged from 13.34 ± 0.092 µm to 17.73 ± 0.217 µm. Swelling study was performed on all the formulation for 24 h and swelling index ranged from 2.95 to 4.27. The particles size of the formulation was found to be 14.04 µm with polydispersity index of 0.701. The mucoadhesion time of the formulation was obtained to be 6 h 19 min. The in vitro release of simvastatin was studied for 12 h and it was found that the microsphere formulation was able to sustain the release of the drug for more than 12 h with 73.2 % drug released at the end of the 12th hour.

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“…Using an X-ray diffractometer (XPERTPRO), Ni-ltered Cu-K radiation, 45 kV, a current of 40 mA radiation, and a vertical goniometer to measure the amount of radiation dispersed in the sample's crystalline regions, an XRD pattern of lyophilized NLCs and pure medication was obtained. At a temperature of 25 °C, diffractograms were produced using a step size of 0.001°C and a detector resolution in 2 (diffraction angle) between 20° and 80° (19).…”

Section: Xrd Studiesmentioning

confidence: 99%

“…DSC thermo grams of the materials GEN, Precirol, PL F-68 and designated lyophilized GEN-NLCs were obtained for drug-lipid compatibility study using DSC (TA Q universal V4.5A analysis instruments). Throughout the temperature range of 30-300 oC, 5-10 mg samples were heated at a rate of 10 0 C min-1., and the samples were sealed in aluminium pans, under nitrogen ow of 60 ml/min (19,20).…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Optimization, Evaluation and Delivery of Genistein Loaded Long Circulating Nanostructured Lipid Carriers for Treatment of Cancer Melanoma Cells

Dewangan

Maurya²,

Sharma

et al. 2022

Preprint

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Genistien is a soy isoflavone phytoestrogen, BCS class IV drug that has been efficacious for treatment of melanoma. Therefore, prepared Genistien loaded nanostructured lipid carriers (GEN-NLCs) for controlled and target delivery to melanoma cells. GEN-NLCs were formulated by solvent diffusion method applied Thogonal Taguchi optimization. Prepared GEN-NLCs were characterized by their physicochemical quality like particle size, zeta potential, morphology (SEM and AFM), entrapment efficiency, in-vitro release, and incompatibility studied such as DSC, and XRD. In-vitro anticancer and cellular uptake studies were accomplished in MTT assay method and A-375 melanoma cell-line by fluorescence-microscopy technique. Nanogel was prepared by incorporating optimized batch of GEN-NLC in methocel and evaluated for particle size and mechanical properties, In-vitro and ex- vivo occlusion studies, in-vitro release and ex-vivo human cadaver skin permeation and retention studies. Prepared GEN-NLCs were found to be a smooth surface with particle size 189.90±2.45 nm, 89.50±4.52% EE, -14.98±1.4mV zeta potential, and sustained release. MTT assay revealed that nanoparticles were 15.37 times more effective against melanoma as compared to pristine drugs. There was no significant change in texture profile of nanogel after incorporating GEN-NLC. Moreover, a significant increase in occlusivity was observed with occlusion factor almost 3.75 times more than control gel at end of 24 h. Ex-vivo studies further confirmed decrease in flux across skin i.e. sustained release pattern of GEN from hydrogel and increased hydration and retention in epidermis. Therefore, topical delivery of GEN-NLC loaded gel showed potential delivery system to target skin epidermis for melanoma cancer cells with enhanced efficacy.

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Mucoadhesive Microspheres of Atorvastatin Calcium: Rational Design, Evaluation and Enhancement of Bioavailability

Cited by 21 publications

References 16 publications

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF CHITOSAN-BASED FLOATING MICROSPHERES FOR TOPOTECAN HCl

Formulation and evaluation of mucoadhesive microspheres of simvastatin using a 23 full factorial approach

Optimization, Evaluation and Delivery of Genistein Loaded Long Circulating Nanostructured Lipid Carriers for Treatment of Cancer Melanoma Cells

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