Development and characterization of a nanoemulsion containing propranolol for topical delivery

Marques, Tatiana Zanela da Silva; Santos-Oliveira, Ralph; Siqueira, Luciana de Oliveira de Betzler; Cardoso, Verônica da Silva; Freitas, Zaida Maria Faria de; Barros, Rita de Cássia da Silva Ascenção; Villa, Ana Lúcia Vazquez; Monteiro, Mariana de Souza de Bustamante Sato; Santos, Elisabete Pereira dos; Ricci, Esther Lopes

doi:10.2147/ijn.s164404

Cited by 54 publications

(29 citation statements)

References 25 publications

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“…31 Compared with the conventional preparation, the sustained release preparation can prolong drug release, improving patient compliance and reducing the frequency of administration. 32,33 The purpose of this study was to establish a high bioavailability and sustained release delivery system for nintedanib based on electrospray technology. The nintedanib solid dispersion was prepared by using electrospray technology to improve its solubility.…”

Section: Introductionmentioning

confidence: 99%

A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology

Liu¹,

Du²,

Li³

et al. 2018

IJN

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BackgroundNintedanib is a new tyrosine kinase inhibitor and growth factor antagonist. It can be used to treat idiopathic pulmonary fibrosis diseases. Nintedanib has poor solubility in the intestinal tract environment, which leads to low bioavailability of just 4.7%.MethodsIn this study, a nintedanib solid dispersion was prepared by electrospray technology with an optimized formula (nintedanib:PVPK30:Soybean lecithin=1:5:0.25) and electrospray parameters (21 kV voltage, 18 cm receiving distance, 0.3 mL/h solution flow rate, 0.5 mm pinhole inner diameter).ResultsThe accumulative release rate of the optimized solid dispersion was more than 60% in 30 minutes and 100% in 60 minutes. The size distribution was uniform and the surface observed with scanning electron microscopy (SEM) was smooth. The DSC and X-ray diffraction results showed that nintedanib existed in the solid dispersion through an amorphous form. Nintedanib solid dispersion sustained-release capsules were prepared to prolong drug release, improve patient compliance and reduce side effects. The accumulative release rate from the sustained release capsules was 35.17%, 54.78%, 70.58%, and 93.93% after 2 h, 6 h, 8 h, and 12 h, respectively, having obvious sustained release effects in vitro. The release behavior of solid dispersion sustained-release capsules in vitro was in accordance with the Ritger-Peppas model. The in vivo studies of nintedanib soft capsules, solid dispersion and nintedanib sustained release capsules in SD rats were investigated; the results showed that the Tmax of the soft capsule, solid dispersion and sustained release capsules were 3 h, 2 h, and 6 h, respectively. The Cmax were 2.945 mg/mL, 5.32 mg/mL, and 3.75 mg/mL, respectively, while the AUC0–24 h was 15.124 mg·h/mL, 23.438 mg·h/mL, and 24.584 mg·h/mL, respectively. The relevant bioavailability of the sustained-release capsules was 162.55% compared to the nintedanib soft capsule and 104.89% compared to the nintedanib solid dispersion.ConclusionThe results suggested superior bioavailability and a sustained-release effect from nintedanib sustained-release capsules, as compared to the reference (commercial nintedanib soft capsule).

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Section: Introductionmentioning

confidence: 99%

A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology

Liu¹,

Du²,

Li³

et al. 2018

IJN

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“…Briefly, 100 mL of water were added to 12 mg of Pluronics F127 and gently stirred using a magnetic bar (Magnetic Stirrer, IKA, C-MAG HS-7) for 3 min and then processed for 3 min using an ultrasonic processor (UP100H, Hielscher, Power: 60%, Cycle: 1) in an ice bath at 10 °C. After the synthesis, transmission electron microscopy (TEM) analysis of the obtained Pluronic F127 Ms was carried out 65 .…”

Section: Formulation Of Investigated Nps Pla/mmt/tra Np Production mentioning

confidence: 99%

Disturbance of cellular homeostasis as a molecular risk evaluation of human endothelial cells exposed to nanoparticles

Wigner

Zieliński

Michlewska

et al. 2021

Sci Rep

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Even though application of nanoparticles in medicine seems to provide unique solutions for drug delivery and diagnosis diseases, understanding interactions between nanoscale materials and biological systems is imperative. Therefore, this study determined the effect of different types of nanoparticles (NPs) on human endothelial cells and examined the types of toxicity responses they can induce. Four different types of NPs were tested (PLA/MMT/TRASTUZUMAB, PLA/EDTMP, PLGA/MDP, and Pluronic F127 MICELLES), representing three putative areas of application: anticancer therapy, scintigraphy, and cosmetology. The experiments were performed on immortalized human umbilical vein endothelial cells (HUVEC-STs). Light contrast phase microscopy as well as cell viability assays showed that only Pluronic F127 MICELLES decreased the number of HUVEC-STs in contrast to PLA/MMT/TRASTUZUMAB, PLA/EDTMP, and PLGA/MDP NPs, which altered cell morphology, but not their confluency. The tested NPs induced not only DNA strand-breaks and alkali-labile sites, but also internucleosomal DNA fragmentation, visualized as a DNA ladder pattern typical of apoptosis. Moreover, generation of free radicals and subsequent mitochondrial membrane potential collapse showed the significance of free radical production during interactions between NPs and endothelial cells. High concentrations of NPs had different degrees of toxicity in human endothelial cells and affected cell proliferation, redox homeostasis, and triggered mitochondrial dysfunction.

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“…The formulations developed are for topical application on the skin; therefore, cytotoxicity studies were performed with skin cells. Studies with human dermal fibroblast culture, ATCC® PCS-201-012™, were chosen because they are sensitive skin cells in relation to formulations of topical administration (Marques et al 2018).…”

Section: Evaluation Of In Vitro Cytotoxicity Of Saccharum Officinarummentioning

confidence: 99%

Development and Characterization of Phytocosmetic Formulations with Saccharum officinarum

Alves

Gomes

et al. 2020

Rev. Bras. Farmacogn.

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Saccharum officinarum L., Poaceae (sugarcane), occurs in tropical and subtropical areas of the planet, and Brazil stands out as the largest producer of sugar and ethanol from sugarcane. In addition, it is rich in phenolic substances, which have antioxidant potential, generating interest in its use in the cosmetic area. The objective of this work was to develop and characterize an emulsion and a nanoemulsion containing S. officinarum fraction. S. officinarum fraction was analyzed through liquid chromatography/electrospray ionization tandem mass spectroscopy (LC-ESI-MS) analysis and in vitro cytotoxicity. The formulations were developed with 10% Tween™ 80, 8% diethylamino hydroxybenzoylhexylbenzoate, 10% octylmethoxycinnamate, 0.3% conserv™, 1% aristoflex™ AVC, 0.4% of S. officinarum fraction, and distilled water. The emulsion was developed by the fusion-emulsification method and nanoemulsion by processing on the Hielscher UP100H Ultrasound for 5 min. The macroscopic aspects, pH, viscosity, mean droplet size, and in vitro FPS were analyzed. Through LC-ESI-MS analysis, it was possible to verify the presence of phenolic substances in the composition of methanol fraction from sugarcane juice and the IC 50 estimated was 21.08 ± 6.43 mg/ml. All formulations presented pH around 5. The emulsion, emulsion with S. officinarum fraction, nanoemulsion, and nanoemulsion with S. officinarum fraction showed a size of 1.68 ± 0.12 μm, 0.58 ± 0.08 μm, 222 ± 1.58 nm, and 195.0 ± 0.53 nm, respectively. The in vitro sun protection factor of the emulsion, emulsion with S. officinarum fraction, nanoemulsion, and nanoemulsion with S. officinarum fraction was 20 ± 5, 30 ± 3, 24 ± 2, and 35 ± 5.6, respectively. The UVA/UVB ratio of all formulations was moderate and presented λc of 370 nm, which is considered a broad-spectrum product. Substances with photoprotective potential can be found in tailings from the sugarcane industry, suggesting that it can be converted into raw materials or innovative cosmetic products.

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Development and characterization of a nanoemulsion containing propranolol for topical delivery

Cited by 54 publications

References 25 publications

A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology

A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology

Disturbance of cellular homeostasis as a molecular risk evaluation of human endothelial cells exposed to nanoparticles

Development and Characterization of Phytocosmetic Formulations with Saccharum officinarum

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