Development and Statistical Optimization of Solid Lipid Nanoparticle Formulations of Fluticasone Propionate

Amasya, Gülin; Sengel-Türk, Ceyda Tuba; Badıllı, Ulya; Tarimci, Nilüfer

doi:10.4274/tjps.galenos.2019.27136

Cited by 4 publications

(4 citation statements)

References 33 publications

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“…Despite the low quantity of FP and SAL in the final formula, it is possible that FP and SAL transformed into amorphous material within the nanoparticles. Similar findings were reported by Amasya et al [ 37 ].…”

Section: Resultssupporting

confidence: 92%

Novel Fluticasone Propionate and Salmeterol Fixed-Dose Combination Nano-Encapsulated Particles Using Polyamide Based on L-Lysine

et al. 2022

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One of the key challenges in developing a dry powder inhaler (DPI) of an inhalable potent fixed-dose combination (FDC) is the ability of the formulation to generate an effective and reproducible aerosol able to reach the lower parts of the lungs. Herein, a one-step approach is presented to expedite the synthesis of nanoaggregates made from a biocompatible and biodegradable polyamide based on L-lysine amino acid employing market-leading active pharmaceutical ingredients (fluticasone propionate (FP) and salmeterol xinafoate (SAL)) for the management of asthma. The nanoaggregates were synthesized using interfacial polycondensation that produced nanocapsules with an average particle size of 226.7 ± 35.3 nm and zeta potential of −30.6 ± 4.2 mV. Differential scanning calorimetric analysis and x-ray diffraction, as well as scanning electron microscopy of the produced FDC, revealed the ability of the produced nanocapsules to encapsulate the two actives and display the best aerodynamic performance. The FDC nanocapsules displayed 88.5% and 98.5% of the emitted dose for FP and SAL, respectively. The fine particle fraction of the nominated dose was superior to the marketed product (Seretide Diskus®, Brentford, United Kingdom). The in-vitro release study showed an extended drug release profile. Our findings suggest that nanoaggregates using polyamides based on L-lysine and interfacial polycondensation can serve as a good platform for pulmonary drug delivery of FDC systems.

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Section: Resultssupporting

confidence: 92%

Novel Fluticasone Propionate and Salmeterol Fixed-Dose Combination Nano-Encapsulated Particles Using Polyamide Based on L-Lysine

et al. 2022

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“…DSC was used to determine the physical characteristics and crystal structure of coenzyme Q10, solid lipids, and coenzyme Q10 NLCs [19]. Meanwhile, the DSC thermogram of tristearin and stearyl alcohol as presented in Figure 1 showed two endothermic peaks, indicating the presence of a crystal structure in tristearin and stearyl alcohol [20,21]. In general, triglycerides and fatty acids exhibit three different polymorphs [22][23][24].…”

Section: Discussionmentioning

confidence: 99%

Development, characterization, molecular docking, and in vivo skin penetration of coenzyme Q10 nanostructured lipid carriers using tristearin and stearyl alcohol for dermal delivery

Aryani

Siswodihardjo

Soeratri

et al. 2021

Journal of Basic and Clinical Physiology and Pharmacology

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Objectives This study aims to develop coenzyme Q10 nanostructured lipid carriers (NLCs) using tristearin and stearyl alcohol as well as isopropyl palmitate (IPP) as solid and liquid lipid respectively for the dermal delivery system. Methods The coenzyme Q10 NLCs were optimized using tristearin, and stearyl alcohol in different concentrations and further characterized by dynamic light scattering (DLS) for particle size, polydispersity index (PDI), zeta potential, differential scanning calorimetry (DSC) and X-ray diffractometry for crystallinity behavior, Fourier transform infrared spectroscopy (FT-IR) for drug-lipid interaction, scanning electron microscopy (SEM) for particle shape, viscometer for viscosity, and pH meter for pH value. Furthermore, entrapment efficiency (EE), drug loading (DL), and skin penetration in vivo were also evaluated while molecular docking was conducted to examine the interaction between coenzyme Q10 and the lipids. Results The coenzyme Q10 NLCs with tristearin-IPP and stearyl alcohol-IPP as lipid matrix had <1,000 nm particle size, <0.3 PDI, less negative than −30 mV zeta potential, about 41% crystallinity index, and about six as the pH value. Moreover, the EE, DL, viscosity, and in vivo skin penetration of the NLCs using tristearin were higher compared to stearyl alcohol, however, the skin penetration depths for both NLCs were not significantly different. Furthermore, the in silico binding energy of coenzyme Q10-tristearin was lower compared to coenzyme Q10-stearyl alcohol. Both of them showed hydrophobic and van der Waals interaction. Conclusions The NLCs of coenzyme Q10 were formulated successfully using tristearin-IPP and stearyl alcohol-IPP for dermal delivery.

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“…The particle size distributions of almost all coenzyme Q10 NLCs were narrow and homogenous, except (F5). It is due to the PDI of Q10 NLCs were <0.3 (Amasya et al, 2020;Öztürk et al, 2020) as shown in Table 2. The zeta potentials of the Q10 NLCs were -21.5 to -56.2 mv, as shown in Table 2.…”

Section: Particle Size Pdi and Zeta Potentialmentioning

confidence: 93%

“…The melting points and enthalpies of the coenzyme NLCs were lower than the melting points and enthalpies of coenzyme Q10 and myristic acid. It was due to that coenzyme Q10 become an amorphous phase and molecularly dispersed into the lipid matrix (Aliasgharlou et al, 2016;Bhattacharyya and Reddy, 2019;Amasya et al, 2020).…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Development, characterization in vitro and in silico of coenzyme Q10 loaded myristic acid with different liquid lipids nanostructured lipid carriers

Aryani¹,

Siswandono²,

Soeratri³

et al. 2021

J Pharm Pharmacogn Res

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Context: Nanostructured lipid carriers can enhance skin penetration of active substances. Coenzyme Q10 is a lipophilic antioxidant, that has poor skin penetration. This limitation is overcome by nanostructured lipid carriers. Aims: To developed coenzyme Q10 nanostructured lipid carriers using myristic acid with various liquid lipids as lipid matrix by in vitro studies and in silico approach for explaining the interaction of coenzyme Q10-lipid at the molecular level. Methods: The coenzyme Q10 nanostructured lipid carriers were prepared using myristic acid as solid lipid with oleic acid, isopropyl myristate, and isopropyl palmitate as liquid lipids using the high shear homogenization method. Then, they were evaluated in physicochemical characteristics by dynamic light scattering, differential scanning calorimetry, Fourier transforms infrared, scanning electron microscopy, spectrophotometry ultraviolet-visible, and pH meter. Furthermore, the in silico studies were conducted using AutoDock 4.2. Results: The coenzyme Q10 nanostructured lipid carriers using myristic acid-oleic acid, myristic acid-isopropyl myristate, and myristic acid-isopropyl palmitate as lipid matrix had the mean particle size, polydispersity index, entrapment efficiency, drug loading, and pH value were less than 300 nm, less than 0.3, more than 80%, about 10%, and about 5.0, respectively. Moreover, molecular docking of coenzyme Q10 and lipid showed hydrogen and hydrophobic bonds. These results supported differential scanning calorimetry and Fourier transforms infrared results. Conclusions: The coenzyme Q10 nanostructured lipid carriers were successfully prepared using myristic acid-oleic acid, myristic acid-isopropyl myristate, and myristic acid-isopropyl palmitate as lipid matrix as well as in silico study could be used for explaining of coenzyme Q10-lipid interaction.

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Development and Statistical Optimization of Solid Lipid Nanoparticle Formulations of Fluticasone Propionate

Cited by 4 publications

References 33 publications

Novel Fluticasone Propionate and Salmeterol Fixed-Dose Combination Nano-Encapsulated Particles Using Polyamide Based on L-Lysine

Novel Fluticasone Propionate and Salmeterol Fixed-Dose Combination Nano-Encapsulated Particles Using Polyamide Based on L-Lysine

Development, characterization, molecular docking, and in vivo skin penetration of coenzyme Q10 nanostructured lipid carriers using tristearin and stearyl alcohol for dermal delivery

Development, characterization in vitro and in silico of coenzyme Q10 loaded myristic acid with different liquid lipids nanostructured lipid carriers

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