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1.
Drug Des Devel Ther ; 16: 1963-1974, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35783198

RESUMO

Introduction: Numerous drugs with potent toxicity against cancer cells are available for treating malignancies, but therapeutic efficacies are limited due to their inefficient tumor targeting and deleterious effects on non-cancerous tissue. Therefore, two improvements are mandatory for improved chemotherapy 1) novel delivery techniques that can target cancer cells to deliver anticancer drugs and 2) methods to specifically enhance drug efficacy within tumors. The loading of inert drug carriers with anticancer agents and peptides which are able to bind (target) tumor-related proteins to enhance tumor drug accumulation and local cytotoxicity is a most promising approach. Objective: To evaluate the anticancer efficacy of Chitosan nanoparticles loaded with human growth hormone hGH fragment 176-191 peptide plus the clinical chemotherapeutic doxorubicin in comparison with Chitosan loaded with doxorubicin alone. Methods: Two sets of in silico experiments were performed using molecular docking simulations to determine the influence of hGH fragment 176-191 peptide on the anticancer efficacy of doxorubicin 1) the binding affinities of hGH fragment 176-191 peptide to the breast cancer receptors, 2) the effects of hGH fragment 176-191 peptide binding on doxorubicin binding to these same receptors. Further, the influence of hGH fragment 176-191 peptide on the anticancer efficacy of doxorubicin was validated using viability assay in Human MCF-7 breast cancer cells. Results: In silico analysis suggested that addition of the hGH fragment to doxorubicin-loaded Chitosan nanoparticles can enhance doxorubicin binding to multiple breast cancer protein targets, while photon correlation spectroscopy revealed that the synthesized dual-loaded Chitosan nanoparticles possess clinically favorable particle size, polydispersity index, as well as zeta potential. Conclusion: These dual-loaded Chitosan nanoparticles demonstrated greater anti-proliferative activity against a breast cancer cell line (MCF-7) than doxorubicin-loaded Chitosan. This dual-loading strategy may enhance the anticancer potency of doxorubicin and reduce the clinical side effects associated with non-target tissue exposure.


Assuntos
Antineoplásicos , Neoplasias da Mama , Quitosana , Hormônio do Crescimento Humano , Nanopartículas , Antineoplásicos/química , Neoplasias da Mama/tratamento farmacológico , Quitosana/química , Quitosana/farmacologia , Doxorrubicina , Feminino , Humanos , Células MCF-7 , Simulação de Acoplamento Molecular , Nanopartículas/química , Peptídeos/uso terapêutico
2.
Pharmaceutics ; 13(7)2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34371776

RESUMO

Breast cancer is the most widespread malignancy in women worldwide. Nanostructured lipid carriers (NLCs) have proven effective in the treatment of cancer. NLCs loaded with imatinib (IMA) (NANIMA) were prepared and evaluated for their in vitro efficacy in MCF-7 breast cancer cells. The hot homogenization method was used for the preparation of NANIMAs. An aqueous solution of surfactants (hot) was mixed with a molten mixture of stearic acid and sesame oil (hot) under homogenization. The prepared NANIMAs were characterized and evaluated for size, polydispersity index, zeta potential, encapsulation efficiency, release studies, stability studies, and MTT assay (cytotoxicity studies). The optimized NANIMAs revealed a particle size of 104.63 ± 9.55 d.nm, PdI of 0.227 ± 0.06, and EE of 99.79 ± 0.03. All of the NANIMAs revealed slow and sustained release behavior. The surfactants used in the preparation of the NANIMAs exhibited their effects on particle size, zeta potential, encapsulation efficiency, stability studies, and release studies. The cytotoxicity studies unveiled an 8.75 times increase in cytotoxicity for the optimized NANIMAs (IC50 = 6 µM) when compared to IMA alone (IC50 = 52.5 µM) on MCF-7 breast cancer cells. In the future, NLCs containing IMA will possibly be employed to cure breast cancer. A small amount of IMA loaded into the NLCs will be better than IMA alone for the treatment of breast cancer. Moreover, patients will likely exhibit less adverse effects than in the case of IMA alone. Consequently, NANIMAs could prove to be useful for effective breast cancer treatment.

3.
PLoS One ; 15(9): e0238458, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32911507

RESUMO

BACKGROUND: Western dietary habits, coupled with a sedentary lifestyle, are potential contributors to the prevalence and rapid increase in the incidence of obesity in Saudi Arabia. This study aimed to investigate the association between students' weight status and their eating behaviors and practices. Another aim was to assess students' awareness of the health risks associated with obesity. METHODS: A cross-sectional survey was conducted among a sample of 416 (53% male and 47% female) undergraduate students, aged 18-26 years old, between January 6 and April 6, 2019, from colleges of Health Sciences at Jazan University in the Kingdom of Saudi Arabia (K.S.A). Students completed a self-administered questionnaire and recorded their measured anthropometric parameters. RESULTS: The prevalence of overweight (20.4%) and obesity (14.9%) were relatively high among the participants. There were statistically significant associations between Body Mass Index (BMI) and the different settings of food consumption (i.e., dining on a table (or) in the Islamic way: squatting on the ground) (p<0.001)). BMI was also associated with students' dietary habits regarding consuming food, snacks, and drinking carbonated beverages while watching television (p<0.001), as well as consuming the same pattern of food/drink while watching television, playing video games on mobile phones or computers (p<0.001). Nearly most of the students were oblivious to the fact that metabolic syndrome, reproductive disorders, respiratory disorders along with liver and gallbladder diseases are some of the health risks associated with obesity. CONCLUSION: The prevalence of obesity and overweight were reasonably high in our study sample and were affected by several factors related to students' eating behaviors and practices. This warrants the need for rigorous and frequent health education interventions on healthy eating behaviors, dietary practices, with an emphasis on the importance of adopting an active, healthy lifestyle.


Assuntos
Comportamento Alimentar/psicologia , Obesidade/psicologia , Estudantes/psicologia , Adolescente , Adulto , Índice de Massa Corporal , Computadores , Estudos Transversais , Dieta/estatística & dados numéricos , Feminino , Educação em Saúde , Humanos , Incidência , Masculino , Obesidade/epidemiologia , Sobrepeso/epidemiologia , Prevalência , Arábia Saudita/epidemiologia , Comportamento Sedentário , Estudantes/estatística & dados numéricos , Inquéritos e Questionários , Televisão , Universidades , Adulto Jovem
4.
Drug Deliv ; 27(1): 622-631, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32329374

RESUMO

NLC containing Gefitinib (NANOGEF) was prepared using stearic acid, sesame oil and surfactants (sodium lauryl sulfate and tween 80). NANOGEFs were evaluated for particle size, polydispersity index (PdI), zeta potential, entrapment efficiency (EE), stability, release studies and cytotoxicity studies (MTT assay). The optimized NANOGEF exhibited particle size of 74.06 ± 9.73 d.nm, PdI of 0.339 ± 0.029 and EE of 99.76 ± 0.015%. The TEM study revealed spherical shape of NANOGEF formulations. The slow and sustained release behavior was exhibited by all NANOGEFs. The effects of surfactants were observed not only on particle size but also on zeta potential, entrapment efficiency, stability and release studies. The MTT assay revealed 4.5 times increase in cytotoxicity for optimized NANOGEF (IC50 = 4.642 µM) when compared with Gefitinib alone (IC50 = 20.88 µM in HCT-116 cells). Thus NANOGEF may be considered as a potential drug delivery system for the cure of colon cancer.


Assuntos
Antineoplásicos/administração & dosagem , Neoplasias do Colo/tratamento farmacológico , Gefitinibe/administração & dosagem , Lipídeos/química , Nanoestruturas/química , Morte Celular , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Células HCT116 , Humanos , Lipídeos/administração & dosagem , Nanoestruturas/administração & dosagem , Tamanho da Partícula
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