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1.
Assay Drug Dev Technol ; 20(6): 274-285, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36121789

RESUMO

Nanoemulsion (NE), a lipid-based drug delivery system, plays an important role in delivering drugs and enhancing bioavailability. They are mainly taken up by the reticuloendothelial system, because of which their bioavailability is diminished, leading to poor therapeutic activity. It is important to protect this delivery system using a coating agent. Thus, we have coated o/w type NE using polyethylene glycol (PEG). The novelty in our study is use of dicarboxylic acid-linked PEG. Furthermore, the spontaneous emulsification method was used in preparation and peg coating, not mentioned previously. After the preparation of NE, various characterization and stability studies were carried out. We have also optimized the ratios for NE and PEG NE by using various concentrations of Smix, PEG, and water. Also, the same has also been plotted in a pseudoternary-phase diagram. As a conclusion, the PEGylation of NE was carried out successfully and may also be used for linking with other ligands because of the presence of COOH group.


Assuntos
Nanopartículas , Emulsões , Lipídeos , Polietilenoglicóis , Água
2.
Curr Pharm Des ; 28(38): 3114-3126, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36173049

RESUMO

Breast cancer is the second leading cause of cancer-related deaths. It is important to target the complex pathways using a suitable targeted delivery system. Targeted delivery systems can effectively act on cancer cells and lead to the annihilation of tumor proliferation. They mainly employ targeting agents like aptamers linked to the formulation. Based on the expression of the receptors on the surface of the cancer cells, suitable aptamers can be developed. AS1411 is one such aptamer that has the ability to bind to the over-expressed nucleolin present in breast cancer cells. Nucleolin is a phosphoprotein that is involved in various aspects, like cell growth, differentiation and survival. Mostly they are found in the nucleolus, nucleus, cytoplasm and cell surface. The shuttling effect of the nucleolin between the nucleus and cytoplasm serves as a bonus for the AS1411 aptamer. Because of the shutting effect, the internalization of the drug compound or chemotherapeutic drug inside the cell can be achieved. In this article, we have discussed nucleolin, anti-nucleolin aptamer, namely, AS1411, and its application in exhibiting various anticancer activities, including apoptosis, anti-angiogenesis, anti-metastasis, stimulation of tumor suppressor (i.e., P53), and inhibition of tumor inducer. Further, the ways of internalization, namely macropinocytosis, are also discussed. Additionally, we have also discussed the superiority of the aptamer compared to the antibodies as well as the limitations of the aptamers. By considering all the above parameters, we hope this aptamer will be effective in the management and eradication of breast cancer cells.


Assuntos
Neoplasias da Mama , Humanos , Feminino , Neoplasias da Mama/tratamento farmacológico , Fosfoproteínas , Proliferação de Células , Apoptose
3.
Exp Gerontol ; 152: 111438, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34098006

RESUMO

Cancer is one of the life-taking diseases worldwide and among cancer-related death; colorectal cancer is the third most. Though conventional methods of treatment are available, multidrug resistance and side effects are predominant. Physicians and scientists are working side by side to develop an effective medicament, which is safe and cost-effective. However, most failures are obtained when focused on the clinical perspective. This review mainly brings out the correlation between the curcumin and its use for the mitigation of colorectal cancer, the use of curcumin as a chemotherapeutic agent, chemosensitizer, and in a combination and synergistic approach. The pharmacokinetics and pharmacodynamics properties of curcumin and its formulation approach helps in giving an idea to develop new approaches for the treatment of colorectal cancer using curcumin.


Assuntos
Antineoplásicos , Neoplasias Colorretais , Curcumina , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Neoplasias Colorretais/tratamento farmacológico , Curcumina/farmacologia , Curcumina/uso terapêutico , Resistência a Múltiplos Medicamentos , Humanos
4.
Med Hypotheses ; 133: 109409, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31581031

RESUMO

Acne vulgaris is a common disease which affects about 85% of the population. Various topical drugs are available, but the retinoid derivatives are mostly taken into consideration. They are used as a first-line treatment drugs. However, they also have few side effects. Whereas, adapalene which is a third generation topical retinoid has fewer side effects compared to other derivatives. In this, we hypothesize that the combination therapy of adapalene and flavonoid could improve the efficacy and thereby it can also decrease the treatment time. Since, flavonoids possess multiple activities we assume that it can improve the action of the drug by showing a synergistic activity. Moreover, when we incorporate these two drugs in nanoemulgel, it can easily penetrate into the skin and produce its therapeutic action. Hence, we assume that if this hypothesis proves to be correct then this method will be an effective one in treating acne (pustule).


Assuntos
Acne Vulgar/tratamento farmacológico , Adapaleno/uso terapêutico , Polifenóis/uso terapêutico , Acne Vulgar/fisiopatologia , Adapaleno/administração & dosagem , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/uso terapêutico , Fármacos Dermatológicos/classificação , Fármacos Dermatológicos/uso terapêutico , Modelos Animais de Doenças , Combinação de Medicamentos , Avaliação Pré-Clínica de Medicamentos , Sinergismo Farmacológico , Emulsões , Feminino , Humanos , Masculino , Camundongos , Nanogéis , Polifenóis/administração & dosagem , Coelhos , Ratos , Receptores do Ácido Retinoico/agonistas
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