DEVELOPMENT OF ORAL NIFEDIPINE-LOADED POLYMERIC NANOCAPSULES: PHYSICOCHEMICAL CHARACTERISATION, PHOTOSTABILITY STUDIES,<i>IN VITRO</i>AND<i>IN VIVO</i>EVALUATION

Tagliari, Monika Piazzon; Granada, Andrea; Silva, Marcos Antônio Segatto; Stulzer, Hellen Karine; Zanetti-Ramos, Betina Giehl; Fernandes, Daniel; Silva, Izabella Thaís; Simões, Cláudia Maria Oliveira; Assreuy, Jamil; Soldi, Valdir

doi:10.5935/0100-4042.20150076

Cited by 4 publications

(3 citation statements)

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“…The transmission electron microscopy (TEM) photomicrographs showed the formation of spherical shaped or nearly spherical nanocapsules. Similar to, Fessi et al 62 and Tagliari et al 75 , the photomicrographs revealed the presence of an opaque film or coat surrounding the oily core for unconjugated (Fig. 6A), and conjugated Eudragit S100 nanocapsules (Fig.…”

Section: Product II N-(6-aminohexyl)-4-methoxybenzamide the Deprotesupporting

confidence: 83%

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

Ramzy

Metwally

Nasr

et al. 2020

Sci Rep

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the biggest challenge in colorectal cancer therapy is to avoid intestinal drug absorption before reaching the colon, while focusing on tumor specific delivery with high local concentration and minimal toxicity. in our work, thymoquinone (tQ)-loaded polymeric nanocapsules were prepared using the nanoprecipitation technique using Eudragit S100 as polymeric shell. Conjugation of anisamide as a targeting ligand for sigma receptors overexpressed by colon cancer cells to Eudragit S100 was carried out via carbodiimide coupling reaction, and was confirmed by thin layer chromatography and 1 H-nMR. tQ nanocapsules were characterized for particle size, surface morphology, zeta potential, entrapment efficiency % (EE%), in vitro drug release and physical stability. A cytotoxicity study on three colon cancer cell lines (HT-29, HCT-116, Caco-2) was performed. Results revealed that the polymeric nanocapsules were successfully prepared, and the in vitro characterization showed a suitable size, zeta potential, EE% and physical stability. TQ exhibited a delayed release pattern from the nanocapsules in vitro. Anisamide-targeted tQ nanocapsules showed higher cytotoxicity against HT-29 cells overexpressing sigma receptors compared to their non-targeted counterparts and free TQ after incubation for 48 h, hence delineating anisamide as a promising ligand for active colon cancer targeting. Sigma receptors are expressed in normal cells of various organs including brain, kidney, liver, immune, endocrine and reproductive organ 1,2. Two distinguished subtypes were recognized and known as sigma-1 and sigma-2 3. Neurosteroids are the likely endogenous ligands for sigma-1 receptors 4 , and N,N-dimethyltryptamine; a natural alkaloid, was also found to be an endogenous ligand for sigma-1 receptors 5,6. A correlation between sigma receptors and diseases such as Parkinson's, Alzheimer's disease and cancer has been proposed 7 , and ligands for sigma-1 receptor were proven to improve various neurodegenerative disorders 8. Sigma-2 receptor is thought to be crucial for cell morphology, survival and differentiation 9. Sigma receptors are overexpressed in cancer cells of various organs 10 including cancers of the brain 11 , lung 12,13 , breast 14 , prostate gland 15 , kidney and colon 16. The tumor environment characterized by oxidative stress, hypoxia, low pH and insufficient supply of glucose and amino acids mediates disruption of endoplasmic reticulum protein folding. This in turn contributes to sigma-1 receptors activation to promote cell survival 7,17. In addition, sigma-2 receptors upregulation in cancerous tissues compared to healthy ones has been widely demonstrated 18,19. Benzamide derivatives demonstrate a high affinity towards sigma receptors 20-22. Anisamide (AA); a small molecular weight benzamide derivative was proven to exhibit high affinity for sigma receptors 23-25. In a review article previously published by our team the use of AA as a targeting ligand in several drug delivery systems was detailed 26. AA-functionalized doxorubicin-loade...

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Section: Product II N-(6-aminohexyl)-4-methoxybenzamide the Deprotesupporting

confidence: 83%

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

Ramzy

Metwally

Nasr

et al. 2020

Sci Rep

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“…Nifedipine was incorporated into polymer nanocapsules formed by surfactants pluronic F68 and polyvinyl alcohol to preserve the drug from degradation. The efficiency of these formations in protecting the drug from light was tested by registering a significant protection [ 59 ]. The photostability of nifedipine in a solid dispersion formulation was also evaluated by dispersing the drug in porous calcium silicate.…”

Section: Photostabilization Approachesmentioning

confidence: 99%

1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies

2019

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The 1,4-dihydropyridine (DHP) drugs are nowadays the most used drugs in the treatment of hypertension. However, all the structures in this series present a significant sensitivity to light, leading to the complete loss of pharmacological activity. This degradation is particularly evident in aqueous solution, so much so that almost all DHP drugs on the market are formulated in solid preparations, especially tablets. The first and main process of photodegradation consists in the aromatization of the dihydropyridine ring, after which secondary processes can take place on the various substituents. A potential danger can result from the formation of single oxygen and superoxide species that can in turn trigger phototoxic reactions. Several strategies for the photostabilisation of DHP drugs have been proposed in recent years, in particular with the aim to formulate these drugs in liquid preparations, as well as to limit any toxicity problems related to light degradation. This review summarizes and describes the main aspects of the studies conducted in recent years to obtain photostable formulations of DHP drugs.

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“…Particle size, zeta potential and entrapment efficiency remained constant during a period of 28 d under light exposure. The pure drug was completely degraded after 4 d while the percentage of drug remaining in the nanocapsules was around 25-30%, suggesting a significant protection of the drug into this matrix [90]. Porous calcium silicate was evaluated for increasing the photostability of nifedipine in a solid dispersion formulation.…”

Section: Photostabilization Approachesmentioning

confidence: 99%

Photodegradation of 1, 4-Dihydropyridine Antihypertensive Drugs: An Updated Review

Luca

Ioele

Spatari

et al. 2018

Int J Pharm Pharm Sci

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ABSTRACT1, 4-dihydropyridine calcium channels blockers (DHPs) are the most commonly used antihypertensive drugs. Unfortunately, these compounds have a significant degradability to light. The oxidation to the pyridine derivative represents the first, and in many cases the only, step of the degradation mechanism. The photodegradation process causes the complete loss of pharmacological activity and may trigger the formation of single and superoxide oxygen species, potentially responsible for phototoxic reactions. Several analytical techniques have been proposed for DHP determination in the presence of their photoproducts. Nowadays, DHPs are all marketed in solid formulations, especially tablets, because photodegradation is particularly fast in solution. Various approaches aimed to protect molecular integrity and therapeutic activity of these drugs from the effects of light are currently studied. This review covers the studies over the last years about photodegradation of the DHPs and the approaches to obtain photostable formulations of these drugs.

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DEVELOPMENT OF ORAL NIFEDIPINE-LOADED POLYMERIC NANOCAPSULES: PHYSICOCHEMICAL CHARACTERISATION, PHOTOSTABILITY STUDIES,IN VITROANDIN VIVOEVALUATION

Cited by 4 publications

References 0 publications

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

1,4-Dihydropyridine Antihypertensive Drugs: Recent Advances in Photostabilization Strategies

Photodegradation of 1, 4-Dihydropyridine Antihypertensive Drugs: An Updated Review

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