Preparation, evaluation and pharmacokinetic studies of spray dried PLGA polymeric submicron particles of simvastatin for the effective treatment of breast cancer

Anzar, Naqueeb; Mirza, Mohd. Aamir; Anwer, Md. Khalid; Khuroo, Tahir; Alshetaili, Abdullah; Alshahrani, Saad; Meena, Jairam; Hasan, Nazia; Talegaonkar, Sushama; Panda, Amulya K.; Iqbal, Zeenat

doi:10.1016/j.molliq.2017.11.081

Cited by 49 publications

(26 citation statements)

References 13 publications

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“…A sharp endothermic peak corresponding to 159.4°C was obtained in the case of free APM, which was found to be much closer to that reported in the literature. 27 An endothermic peak could be seen in PLGA NPs (F1 and F2) at 159.4°C with reduced intensity compared to that of pure APM. This comparison suggested that APM exists in a partially crystalline form and did not encapsulate the drug completely; this might be due to less amount of PLGA polymer used in F1 and F2 PLGA NPs.…”

Section: Dsc Studiesmentioning

confidence: 96%

“…The XRD pattern of pure APM showed several characteristic intense peaks at 10.08° 2θ, 12.38° 2θ, 13.48° 2θ, 20.82° 2θ, 22.50° 2θ, 24.10° 2θ, 24.66° 2θ, and 26.96° 2θ, which was found much closer to the values reported in the literature. 27 However, these peaks were absent or were less peak intensity in the APM-loaded PLGA-NPs. This reduction in the crystallinity of the precipitated PLGA NPs clearly confirmed the encapsulation of APM in the PLGA polymer.…”

Section: Powder Xrd Studiesmentioning

confidence: 97%

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<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

Anwer

Mohammad

Ezzeldin

et al. 2019

IJN

Self Cite

113

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Background Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of −43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment.

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Section: Dsc Studiesmentioning

confidence: 96%

Section: Powder Xrd Studiesmentioning

confidence: 97%

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

Anwer

Mohammad

Ezzeldin

et al. 2019

IJN

Self Cite

113

View full text Add to dashboard Cite

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“…Obviously, smaller droplets are favored by a smaller spray mesh. The submicron particle size is typically reached when using a 4.0 μm spray mesh and diluted solutions of about 0.1 to 1% (w/v), as demonstrated Influence of the main process parameters in nano spray drying ( / strong increasing/decreasing influence, / weak increasing/ decreasing influence, -minimal or no influence) Adapted from Arpagaus et al 2017Nano spray drying process parameter table ( / strong increasing/decreasing influence, ↑/↓ weak increasing/decreasing influence, -minimal or no influence) in several studies (Amsalem et al 2017;Anzar et al 2018;Beck-Broichsitter et al 2012, 2015aBege et al 2013;Panda et al 2016;Schafroth et al 2012). The organic solvents typically used in the nano spray drying of PLA/PLGA biopolymers are mainly: (Schafroth et al 2012).…”

Section: Influence Of Process Parameters On Powder Propertiesmentioning

confidence: 96%

“…E Nano-in-nanoparticles made of PEG-PLGA (100 kDa) and PLGA (100 kDa) loaded with human serum albumin primary nanoparticles containing siRNA (Amsalem et al 2017). F Simvastatin-loaded PLGA submicron particles for the treatment of breast cancer (Anzar et al 2018). G Composite particle fab-ricated from aqueous suspension containing sildenafil-loaded PLGA nanoparticles (Beck-Broichsitter et al 2012).…”

Section: Applications Of Nano Spray Dried Pla/plga Biopolymersmentioning

confidence: 99%

PLA/PLGA nanoparticles prepared by nano spray drying

Arpagaus

2019

J. Pharm. Investig.

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Background Spray drying is a relatively simple, fast, reproducible and scalable drying technology that is suitable for drying heat-sensitive biopharmaceutical compounds. In view of the rapid progress of nanoencapsulation technologies in the pharmaceutical sector, nano spray drying is used in research to improve the powder formulation and release of active ingredients. The Nano Spray Dryer B-90 of the Swiss company Büchi Labortechnik AG extends the size of the powder particles produced into the nanometer scale with narrow size distributions and high encapsulation efficiency. Area covered This study explains the special nano spray drying technology and discusses the influence of the respective process parameters on the powder properties. Applications of nano spray drying for the formulation and encapsulation of active ingredients in PLA/PLGA biopolymers are investigated and discussed. Optimized process parameters for the application of nano spray drying of similar substances are presented. Expert opinion The analyzed studies show the possibility of producing PLGA particles from approx. 2 μm to below 200 nm by nano spray drying, as well as the encapsulation of various active ingredients in spherical particles and nano-in-nanoparticle composite structures made of PLGA polymers for controlled drug delivery systems. The researched applications are primarily in the therapeutic field, such as the treatment of inhalation diseases, inflammations, cancer, immune diseases, genetic disorders, the regulation of vasodilatation or the surface coating of medical implants with biocompatible PLGA nanoparticles.

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“…simvastatin loaded PLGA particles), or lung cancer (e.g. methotrexate, carboplatin in gelatine, or paclitaxel) [90,91,[105][106][107][108],…”

Section: Applications Of Nano Spray Dried Pharmaceuticals On the Labomentioning

confidence: 99%

Pharmaceutical Particle Engineering via Nano Spray Drying - Process Parameters and Application Examples on the Laboratory-Scale

Arpagaus¹

2018

Int J Med Nano Res

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Spray drying plays a crucial role in the processing of pharmaceutical products such as pills, capsules, and tablets as it is used to convert drug-containing liquids into dried powdered forms. Nano spray drying is in particular used to improve drug formulation by encapsulating active ingredients in polymeric wall materials for protection and delivering the drugs to the right place and time in the body. The nano spray dryer developed in the recent years extends the spectrum of produced powder particles to the submicron-and nanoscale with very narrow size distributions and sample quantities in the milligram scale at high product yields. This enables the economical use of expensive active pharmaceutical ingredients and pure drugs. The present paper explains the concept of nano spray drying in the laboratory-scale and discusses the influence of the main process parameters on the final powder properties like particle size, morphology, encapsulation efficiency, and drug loading. Application results of nano spray drying for the formulation and encapsulation of different drugs are reviewed.

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Preparation, evaluation and pharmacokinetic studies of spray dried PLGA polymeric submicron particles of simvastatin for the effective treatment of breast cancer

Cited by 49 publications

References 13 publications

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

PLA/PLGA nanoparticles prepared by nano spray drying

Pharmaceutical Particle Engineering via Nano Spray Drying - Process Parameters and Application Examples on the Laboratory-Scale

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