Formulation of Chitosan-Coated Brigatinib Nanospanlastics: Optimization, Characterization, Stability Assessment and In-Vitro Cytotoxicity Activity against H-1975 Cell Lines

Zaki, Randa Mohammed; Alfadhel, Munerah M.; Alshahrani, Saad; Alsaqr, Ahmed; Al-Kharashi, Layla A.; Anwer, Md. Khalid

doi:10.3390/ph15030348

Cited by 12 publications

(4 citation statements)

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“…Furthermore, the 50 µg/mL dose significantly decreased cell viability compared to other doses of the SIM suspension and unloaded cubosomes. These results suggest that the SIM-cubosomal formula had a considerable effect on breast cancer cells, which could be attributed to the increased cellular uptake of SIM-loaded cubosomes compared to the SIM suspension [ 49 , 50 ].…”

Section: Resultsmentioning

confidence: 99%

Fabrication and Assessment of Orodispersible Tablets Loaded with Cubosomes for the Improved Anticancer Activity of Simvastatin against the MDA-MB-231 Breast Cancer Cell Line

et al. 2023

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Various factors limit the use of simvastatin as an anticancer drug. Therefore, this study aimed to analyse simvastatin (SIM)-loaded cubosome efficacy against breast cancer. SIM-loaded cubosomes were prepared using the emulsification method using different glyceryl monooleate, Pluronic F127 (PF-127), and polyvinyl alcohol (PVA) ratios. The best cubosomal formula was subjected to an in vitro cytotoxicity analysis using the human breast cancer cell line, MDA-MB-231 (MDA) (ATCC, HTB-26), and formulated as oral disintegrating tablets through direct compression. PF-127 and PVA positively affected drug loading, and the entrapment efficiency percentage of different SIM-cubosomal formulations ranged from 33.52% to 80.80%. Vesicle size ranged from 181.9 ± 0.50 to 316.6 ± 1.25 nm. PF-127 enhanced in vitro SIM release from cubosome formulations due to its solubilising action on SIM. The in vitro dissolution analysis indicated that SIM exhibited an initial dissolution of 10.4 ± 0.25% within the first 5 min, and 63.5 ± 0.29% of the loaded drug was released after 1 h. Moreover, cubosome formula F3 at 25 and 50 µg/mL doses significantly decreased MDA cell viability compared to the 12.5 µg/mL dose. The untreated SIM suspension and drug-free cubosomes at all doses had no significant influence on MDA cell viability compared to the control.

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Section: Resultsmentioning

confidence: 99%

Fabrication and Assessment of Orodispersible Tablets Loaded with Cubosomes for the Improved Anticancer Activity of Simvastatin against the MDA-MB-231 Breast Cancer Cell Line

et al. 2023

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“…When examining the stability of vesicles, ZP is a key physical property. Therefore, ZP was employed to foretell the stability of the nanovesicles [ 50 ]. The ZP range of the niosomes ranged from −21.59 to −62.87 mV.…”

Section: Resultsmentioning

confidence: 99%

Preparation and Characterization of Patch Loaded with Clarithromycin Nanovesicles for Transdermal Drug Delivery

Alkilani

Musleh

Hamed

et al. 2023

JFB

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Clarithromycin (CLR), categorized as a Biopharmaceutical Classification System class II drug, has several gastrointestinal tract side effects and an extremely unpalatable bitter taste. The current study aimed to design transdermal patch-embedded CLR niosomes to overcome the aforementioned CLR-related challenges. Various niosomal formulations were successfully fabricated and characterized for their morphology, size, in vitro release, and antimicrobial efficacy. Subsequently, the CLR niosomes were loaded into transdermal patches using the solvent casting method. The polydispersity index of the niosomes ranged from 0.005 to 0.360, indicating the uniformity of the niosomes. The encapsulating efficiency (EE)% varied from 12 to 86%. The optimal Chol: surfactant ratio for drug release was found to be 0.5:1. In addition, the encapsulation of CLR into niosomal nanovesicles did not reduce the antibacterial activity of the CLR. The niosomal patch had a significantly higher permeability coefficient of CLR than the conventional patch. In addition to that, a shear-thinning behavior was observed in the niosomal gels before loading them into a niosomal patch. The flux (Jss) of the niosomal patch was significantly higher than the conventional patch by more than 200 times. In conclusion, niosome-based transdermal patches could be a promising method for the transdermal drug delivery of class II drugs and drugs experiencing GIT side effects.

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“…Concerning the impact of time of sonication X4, it was concluded that by reducing the time of sonication from 15 min to 10 min the EE% significantly amplified, possibly because of decreasing the leakage of LORA to the exterior aqueous medium throughout disruption then nanovesicles re-aggregation instead of encapsulation (Zaki et al, 2022 ). On the other hand, the effect of X1: solid to liquid lipid ratio on EE% of LORA-NLCs, displayed a non-significant impact ( P > 0.05).…”

Section: Resultsmentioning

confidence: 99%

“…Additionally, sonication Time (min) ( P < .0001) significantly affected zeta potential values. Obviously, the time of sonication had impacted negatively the values of zeta potential, where increasing the sonication time led to a decrease in the ZP values and hence, a decrease in the stability of the dispersion system (Zaki et al, 2022 ). Alternatively, the X1: solid to liquid lipid ratio was found to show no significant effect on ZP ( P = .2711).…”

Section: Resultsmentioning

confidence: 99%

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

et al. 2022

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Loratadine (LORA), is a topical antihistamine utilized in the treatment of ocular symptoms of COVID-19. The study aimed to develop a Loratadine Nanostructured Lipid Carriers Ocugel (LORA-NLCs Ocugel), enhance its solubility, trans-corneal penetrability, and bioavailability. full-factorial design was established with 2 4 trials to investigate the impact of several variables upon NLCs properties. LORA-NLCs were fabricated by using hot melt emulsification combined with high-speed stirring and ultrasonication methods. All obtained formulae were assessed in terms of percent of entrapment efficiency (EE%), size of the particle (PS), zeta potential (ZP), as well as in-vitro release. Via using Design Expert® software the optimum formula was selected, characterized using FTIR, Raman spectroscopy, and stability studies. Gel-based of optimized LORA-NLCs was prepared using 4% HPMC k100m which was further evaluated in terms of physicochemical properties, Ex-vivo, and In-vivo studies. The optimized LORA-NLCs, comprising Compritol 888 ATO ® , Labrasol ® , and Span ® 60 showed EE% of 95.78 ± 0.67%, PS of 156.11 ± 0.54 nm, ZP of −40.10 ± 0.55 Mv, and Qh6% of 99.67 ± 1.09%, respectively. Additionally, it illustrated a spherical morphology and compatibility of LORA with other excipients. Consequently, gel-based on optimized LORA-NLCs showed pH (7.11 ± 0.52), drug content (98.62%± 1.31%), viscosity 2736 cp, and Q12% (90.49 ± 1.32%). LORA-NLCs and LORA-NLCs Ocugel exhibited higher ex-vivo trans-corneal penetrability compared with the aqueous drug dispersion. Confocal laser scanning showed valuable penetration of fluoro-labeled optimized formula and LORA-NLCs Ocugel through corneal. The optimized formula was subjected to an ocular irritation test (Draize Test) that showed the absence of any signs of inflammation in rabbits, and histological analysis showed no effect or damage to rabbit eyeballs. C max and the AUC 0–24 were higher in LORA-NLCs Ocugel compared with pure Lora dispersion-loaded gel The research findings confirmed that NLCs could enhance solubility, trans-corneal penetrability, and the bioavailability of LORA.

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Formulation of Chitosan-Coated Brigatinib Nanospanlastics: Optimization, Characterization, Stability Assessment and In-Vitro Cytotoxicity Activity against H-1975 Cell Lines

Cited by 12 publications

References 50 publications

Fabrication and Assessment of Orodispersible Tablets Loaded with Cubosomes for the Improved Anticancer Activity of Simvastatin against the MDA-MB-231 Breast Cancer Cell Line

Fabrication and Assessment of Orodispersible Tablets Loaded with Cubosomes for the Improved Anticancer Activity of Simvastatin against the MDA-MB-231 Breast Cancer Cell Line

Preparation and Characterization of Patch Loaded with Clarithromycin Nanovesicles for Transdermal Drug Delivery

Fabrication of nanostructured lipid carriers ocugel for enhancing Loratadine used in treatment of COVID-19 related symptoms: statistical optimization, in-vitro, ex-vivo, and in-vivo studies evaluation

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