Amorphous Nanoparticulate Formulation of Sirolimus and Its Tablets

Shen, Yu-Dong; Li, Xingya; Le, Yuan

doi:10.3390/pharmaceutics10030155

Cited by 16 publications

(19 citation statements)

References 35 publications

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“…Today, nanomaterials play one of the most important roles in the research and development of modern pharmaceutics [1,2,3]. New material processing procedures [4,5,6,7,8], combined with different kinds of raw materials [9,10,11,12,13] and novel innovative strategies for constructing functional products [14,15,16,17,18], are frequently introduced into this application field for providing efficacious drug delivery and enhancing the therapeutic effects of active pharmaceutical ingredients (APIs). Among them, electrohydrodynamic atomization (EHDA) is a popular technique for creating nanoproducts, which mainly includes electrospraying and electrospinning.…”

Section: Introductionmentioning

confidence: 99%

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

Huang

Hou

et al. 2019

Pharmaceutics

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In pharmaceutical nanotechnology, the intentional manipulation of working processes to fabricate nanoproducts with suitable properties for achieving the desired functional performances is highly sought after. The following paper aims to detail how a modified coaxial electrospraying has been developed to create ibuprofen-loaded hydroxypropyl methylcellulose nanoparticles for improving the drug dissolution rate. During the working processes, a key parameter, i.e., the spreading angle of atomization region (θ, °), could provide a linkage among the working process, the property of generated nanoparticles and their functional performance. Compared with the applied voltage (V, kV; D = 2713 − 82V with RθV2 = 0.9623), θ could provide a better correlation with the diameter of resultant nanoparticles (D, nm; D = 1096 − 5θ with RDθ2 = 0.9905), suggesting a usefulness of accurately predicting the nanoparticle diameter. The drug released from the electrosprayed nanoparticles involved both erosion and diffusion mechanisms. A univariate quadratic equation between the time of releasing 95% of the loaded drug (t, min) and D (t = 38.7 + 0.097D − 4.838 × 105D2 with a R2 value of 0.9976) suggests that the nanoparticle diameter has a profound influence on the drug release performance. The clear process-property-performance relationship should be useful for optimizing the electrospraying process, and in turn for achieving the desired medicated nanoparticles.

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Section: Introductionmentioning

confidence: 99%

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

Huang

Hou

et al. 2019

Pharmaceutics

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“…The preparation procedure of nanoparticle samples and even the presence of other components such as Kodia-PC seems to slightly affect the melting transition of the polymeric material, being the melting peak for all nanoparticle samples more broadly, and shifted to the lowest temperature (54-55 • C) compared to the raw copolymer. Moreover, in the thermogram of drug-loaded samples, the peak related to the melting point of Rapa is absent, demonstrating that the drug entrapment in the polymeric-based nanoparticle sample showed a different state, such as an amorphous state or disordered-crystalline phase of molecular dispersion or solid solution within the polymer matrix, as other authors have recently reported for Rapa or other molecules [35][36][37]. The thermograms did not reveal any degradation of materials in the range of tested temperature.…”

Section: Thermal Analysismentioning

confidence: 62%

Rapamycin-Loaded Polymeric Nanoparticles as an Advanced Formulation for Macrophage Targeting in Atherosclerosis

et al. 2021

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Recently, rapamycin (Rapa) represents a potential drug treatment to induce regression of atherosclerotic plaques; however, its use requires site-specific accumulation in the vessels involved in the formation of the plaques to avoid the systemic effects resulting from its indiscriminate biodistribution. In this work, a stable pharmaceutical formulation for Rapa was realized as a dried powder to be dispersed extemporaneously before administration. The latter was constituted by mannitol (Man) as an excipient and a Rapa-loaded polymeric nanoparticle carrier. These nanoparticles were obtained by nanoprecipitation and using as a starting polymeric material a polycaprolactone (PCL)/α,β-poly(N-2-hydroxyethyl)-dl-aspartamide (PHEA) graft copolymer. To obtain nanoparticles targeted to macrophages, an oxidized phospholipid with a high affinity for the CD36 receptor of macrophages, the 1-(palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine (KOdia-PC), was added to the starting organic phase. The chemical–physical and technological characterization of the obtained nanoparticles demonstrated that: both the drug loading (DL%) and the entrapment efficiency (EE%) entrapped drug are high; the entrapped drug is in the amorphous state, protected from degradation and slowly released from the polymeric matrix; and the KOdia-PC is on the nanoparticle surface (KP-Nano). The biological characterization demonstrated that both systems are quickly internalized by macrophages while maintaining the activity of the drug. In vitro studies demonstrated that the effect of KP-Nano Rapa-loaded, in reducing the amount of the Phospo-Ser757-ULK1 protein through the inhibition of the mammalian target of rapamycin (mTOR), is comparable to that of the free drug.

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“…This demonstrated that the crystalline peaks of the dye nanoparticles were significantly weakened and became an almost amorphous state. It is assumed that poorly water-soluble particles in amorphous state usually exhibit a faster dissolution rate in aqueous solutions [30,31]. In addition, the wetting property of nanoparticles with water was also studied.…”

Section: Resultsmentioning

confidence: 99%

Preparation of Aqueous Nanodispersions of Disperse Dye by High‐Gravity Technology and Spray Drying

Yin

Xu²,

et al. 2020

Chem Eng & Technol

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Disperse dyes are poorly water‐soluble and difficult to stably disperse in an aqueous medium, which greatly limits their application in dyeing synthetic fibers. Micronization can solve this problem. Herein, a facile way to prepare stable aqueous nanodispersions of disperse dye (C.I. disperse yellow 54) is presented by combining high‐gravity antisolvent precipitation in a rotating packed bed (RPB) with spray drying. The as‐prepared product had an average particle size of 120 nm, which could be readily redispersed in water. Compared with raw dye, the wettability and dispersibility of disperse dye nanoparticles were remarkably improved. Furthermore, the dyeing properties of the nanodispersions were obviously better than those of the commercial dye, which was micronized by ball milling.

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Amorphous Nanoparticulate Formulation of Sirolimus and Its Tablets

Cited by 16 publications

References 35 publications

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

Rapamycin-Loaded Polymeric Nanoparticles as an Advanced Formulation for Macrophage Targeting in Atherosclerosis

Preparation of Aqueous Nanodispersions of Disperse Dye by High‐Gravity Technology and Spray Drying

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