Inorganic Nanoparticles: An Alternative Therapy to Combat Drug Resistant Infections

Gupta, Monika

doi:10.22159/ijpps.2021v13i8.42643

Cited by 9 publications

(5 citation statements)

References 179 publications

(170 reference statements)

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“…β-Cyclodextrin (β-CD; polymer) based NSs were prepared in our laboratory by using diphenyl carbonate as a cross-linking by ultrasoundassisted method for fabrication of Entrectinib. β-CD was dissolved in dimethyl formamide, to which diaryl carbonate was added and was left for completion of the reaction and formation of NSs [13].…”

Section: Preparation Of Entrectinib Nssmentioning

confidence: 99%

Determination of in Vitro Cytotoxicity of Entrectinib and Pemigatinib Nanosponges Tablets on a 498, McF-7 and Panc-1 Cell Lines

MAMATHA,

D. V. R. N.

2024

Int J Pharm Pharm Sci

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Objective: The aim of this study was to improve the oral solubility of Pemigatinib and Entrectinib through incorporation into nanosponges (NSs), and further the cytotoxic potential of optimized formulations of NSs on A498, MCF-7, and PANC-1 cell lines in the MTT based Cell proliferation assay was analyzed. Methods: In the current study Pemigatinib and Entrectinib were formulated in to NS tablets and cytotoxicity was determined by using A498, MCF-7, and PANC-1 cell lines. The optimized NS formulation was determined prepared into a tablet dosage form, which further was evaluated for physical parameters and in vitro drug release study. For cytotoxicity studies, MTT assay was conducted for these formulations, IC50 values were calculated for the tested compound and compared with 5-Fluorouracil. Results: The optimized formulation was evaluated for physical parameters and in vitro drug release study, the results were satisfactory. The IC50 of Entrectinib NS, Pemigatinib NS and 5-Fluorouracil, against A498 cell line was 26.34, 85.24 and 15.24 µg/ml, respectively. The IC50 of Entrectinib NS, Pemigatinib NS and 5-Fluorouracil, against MCF-7 cell line was 71.54, 35.48 and 24.56 µg/ml, respectively. The IC50 of Entrectinib NS, Pemigatinib NS and 5-Fluorouracil, against PANC-1 cell line was 35.14, 22.54 and 22.54 µg/ml, respectively. It was observed that the IC50 of drug-loaded NS was higher than the comparator drug and these enter the cells by active transport and induce cytotoxicity to the cells. Conclusion: The overall results from the studies suggest that Entrectinib NS and Pemigatinib NS provided efficient cytotoxic effects, which could play a significant role in the percentage cell death.

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Section: Preparation Of Entrectinib Nssmentioning

confidence: 99%

Determination of in Vitro Cytotoxicity of Entrectinib and Pemigatinib Nanosponges Tablets on a 498, McF-7 and Panc-1 Cell Lines

MAMATHA,

D. V. R. N.

2024

Int J Pharm Pharm Sci

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“…NBDDS have sparked a lot of research interest in recent years because of the potential benefits, such as improving lipophilic drug solubility, increasing permeability, improving drug stability, controlling drug distribution and elimination, and targeting drug delivery to a specific site. Several NBDDS have been produced, including nanocrystals, nanoemulsions, nanosponges (NSs), nanobubbles, liposomes, polymeric micelles, polymeric nanoparticles, and inorganic nanocarriers [9,10].…”

Section: Introductionmentioning

confidence: 99%

Development, Characterization and Evaluation of Entrectinib Nanosponges Loaded Tablets for Oral Delivery

PALANATI,

BHIKSHAPATHI

2023

Int J App Pharm

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Objective: As Entrectinib is a lipophilic, basic, moderately permeable molecule with strongly pH-dependent solubility with antitumor activity in advanced and metastatic solid tumors, the current study was designed to improve the oral solubility of Entrectinib through incorporation into nanosponges tablets (NSs). Methods: Box-Behnken Design was used to optimize the independent variables of β-Cyclodextrin (β-CD) NSs formation. β-CD NSs were prepared by an ultrasound-assisted method using diphenyl carbonate as cross-linking agent, which were later characterized and formulated into tablets by wet granulation method. The prepared tablets were evaluated for the physico-chemical properties and in vitro release of the drug. Results: A series of fifteen experiments were performed based on the experimental runs generated from a three-factor, three-level Box–Behnken design (BBD). The range of mean particle size was 149-294 nm, the range for encapsulation efficiency % was 65.4%-87.3%, and the value for polydispersity index was 0.437. The zeta potential for the optimized formulation was found to be 38.1 Mv. The drug and excipients were compatibles as confirmed by Fourier Transformed Infrared (FTIR) Spectroscopy and Differential Scanning Calorimetry (DSC) studies. Scanning Electron Microscopic (SEM) analysis confirmed that the Entrectinib has successfully entrapped in the core of polymer. In vitro release of the Entrectinib-loaded NSs tablets (six compositions) were compared with a marked product and satisfactory results were obtained. It was observed that rapid dissolution occurred in 0.1 N HCl for first 2 h (15.64±1.52% vs. 12.67±1.89%) and 98.94±2.43% of drug release was observed in Entrectinib loaded NSs and 91.78±1.37% in marketed product in 24 h. The prepared formulations were stable during 6 mo stability study period. Conclusion: The study results studies of Entrectinib NS tablets indicated rapid dissolution due to changed solubility properties of the drug, compared to pure drug meeting the set objective of enhanced absorption. The formulated Entrectinib-loaded NSs can be beneficial in the treatment of cancers.

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“…Numerous NBDDS have been produced, including nanocrystals, nanoemulsions, nanosponges (NSs), nanobubbles, liposomes, micelles, nanoparticles, & inorganic nanocarriers. 7,8 Many studies have shown that NS dosage forms can amplify solubility and thus oral availability of weakly soluble medicines. 9 They shield molecular compounds from degradation and these have high selectivity, biocompatibility, degradability, and extended release behavior which are used in cancer therapy.…”

Section: Introductionmentioning

confidence: 99%

Preparation and In-vitro Evaluation of Pemigatinib Nanosponges Tablets by Box-Behnken Design

Mamatha,

Bhikshapathi

2023

IJPQA

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Objective: Pemigatinib depicted antitumor action in complex and metastatic tumors and it’s a hydrophobic compound having strong pH-reliant solubility. The current work was designed to improve oral solubility of pemigatinib by incorporating into nanosponges (NSs). Methods: Box-Behnken Design optimized the independent parameters of polystyrene NSs formation. Polystyrene NSs were prepared by ultrasound-assisted method using diaryl carbonate as cross-linking agent, which were later characterized and formulated into tablets. Tablets got screened for the respective quality attributes. Results: A number of tests were carried out from the test runs generated by a three-factor, three-level BBD. The range of mean PS was 153 to 316 nm, the range for encapsulation efficiency% was 68.2 to 91.4%, and the value for PDI was 0.273 to 0.445. ZP for the finalized formula was determined to be -29.1 mV. The drug and excipients were compatible as confirmed by FTIR studies. SEM study confirmed that pemigatinib has successfully entrapped in interior of the polymer. In-vitro examination of the pemigatinib loaded NSs tablets were compared with a marked product and satisfactory results were obtained (98.74 ± 2.65% vs. 93.73 ± 1.06%). The prepared formulations were stable during 6 month stability study period. Conclusion: The study findings for pemigatinib NS tablets demonstrated quick dissolution since the changed solubility qualities of the drug, satisfying the intended objective of increased absorption. Formulated pemigatinib-loaded NSs can be beneficial in the treatment of cancers

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Inorganic Nanoparticles: An Alternative Therapy to Combat Drug Resistant Infections

Cited by 9 publications

References 179 publications

Determination of in Vitro Cytotoxicity of Entrectinib and Pemigatinib Nanosponges Tablets on a 498, McF-7 and Panc-1 Cell Lines

Determination of in Vitro Cytotoxicity of Entrectinib and Pemigatinib Nanosponges Tablets on a 498, McF-7 and Panc-1 Cell Lines

Development, Characterization and Evaluation of Entrectinib Nanosponges Loaded Tablets for Oral Delivery

Preparation and In-vitro Evaluation of Pemigatinib Nanosponges Tablets by Box-Behnken Design

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