Development and evaluation of decorated aceclofenac nanocrystals

Park, Jeong-Joo; Meghani, Nilesh M.; Choi, Jin‐Seok; Lee, Beom‐Jin

doi:10.1016/j.colsurfb.2016.03.022

Cited by 30 publications

(7 citation statements)

References 28 publications

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“…In previous studies, surface-modified drug crystals showed faster drug release than pure drugs did 15,51,52. Drug NCs have smaller size than pure drug.…”

Section: Resultsmentioning

confidence: 88%

“…Various types of NPs have been developed for drug delivery, including polymeric NPs,11 solid lipid NPs (SLN),12 liposome,13 self-assembly NPs,14 and drug nanocrystals (NCs) 15. NPs can be surface modified using targeting ligands, such as transferrin,16 hyaluronic acid,17 trastuzumab,18 and peptides,19 to improve their tumor targeting and cellular internalization.…”

Section: Introductionmentioning

confidence: 99%

“…Recently, significant advancement has been made in the field of drug NCs because of numerous studies on the development of NCs of drugs such as DTX,30 PTX,31 curcumin,32 aceclofenac,15 valsartan,33 and quercetin 34. Drug NCs are usually prepared by two methods, top-down and bottom-up methods 35,36.…”

Section: Introductionmentioning

confidence: 99%

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Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Choi¹,

Park²

2016

DDDT

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The purpose of this study was to develop the surface modification of docetaxel nanocrystals (DTX-NCs) with apo-Transferrin human (Tf) for improving the cellular uptake and cytotoxicity of DTX. DTX-NCs were prepared by a nanoprecipitation method, and the surface modified with Tf by an adsorption method (Tf-DTX-NCs). The morphology and particle size of DTX-NCs and Tf-DTX-NCs were characterized using a field emission scanning electron microscope and zetasizer. An in vitro drug release study was performed in phosphate-buffered saline containing 0.5% (w/v) Tween 80 for 24 hours. Cellular uptake was studied at 0.5, 1, and 2 hours. A cytotoxicity study was performed using the A549 (human lung cancer) cell line after 24-, 48-, and 72-hour treatments. The mean sizes were 295±97 and 398±102 nm for DTX-NCs and Tf-DTX-NCs, respectively. Tf-DTX-NCs and DTX-NCs exhibited rapid drug release, whereas DTX (pure) was slowly released. Tf-DTX-NCs showed higher cellular uptake than DTX-NCs in confocal microscopic and quantitative studies. Moreover, at DTX concentration of 100 µg/mL, Tf-DTX-NCs (82.6%±0.8%) showed higher cytotoxicity than DTX-NCs (77.4%±4.1%) and DTX (pure; 20.1%±4.6%) for 72-hour treatment. In conclusion, Tf-DTX-NCs significantly improved the cellular uptake and cytotoxicity of DTX in the A549 cell line.

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“…In previous studies, surface-modified drug crystals showed faster drug release than pure drugs did 15,51,52. Drug NCs have smaller size than pure drug.…”

Section: Resultsmentioning

confidence: 88%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Choi¹,

Park²

2016

DDDT

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“…The size was controlled by probe-sonication. 29 There is another literature on ACF-Soluplus ® nanocomposites by high-shear homogenization using a probe sonicator. 31 Nevertheless, most of these methods use many excipients that may be an economic burden.…”

Section: Introductionmentioning

confidence: 99%

“…24 Scientists have worked on improving the solubility of ACF by various approaches like solid dispersion, 9,25 cyclodextrin complexes, 26,27 chitosan nanoparticles, 28 and nanocrystals. 29,30 Recently, Park et al prepared decorated ACF nanocrystals using nanoprecipitation technique. The size was controlled by probe-sonication.…”

Section: Introductionmentioning

confidence: 99%

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

Narayan¹,

Pednekar²,

Bhuyan³

et al. 2017

IJN

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The aim of the present work was to tackle the solubility issue of a biopharmaceutics classification system (BCS)-II drug, aceclofenac. Although a number of attempts to increase the aqueous solubility have been made, none of the methods were taken up for scale-up. Hence size reduction technique by a top-down approach using wet milling process was utilized to improve the solubility and, consequently, the dissolution velocity of aceclofenac. The quality of the final product was ensured by Quality by Design approach wherein the effects of critical material attributes and critical process parameters were assessed on the critical quality attributes (CQAs) of nanocrystals. Box–Behnken design was applied to evaluate these effects on critical quality attributes. The optimized nanocrystals had a particle size of 484.7±54.12 nm with a polydispersity index (PDI) of 0.108±0.009. The solid state characterization of the formulation revealed that the crystalline nature of the drug was slightly reduced after the milling process. With the reduced particle size, the solubility of the nanocrystals was found to increase in both water and 0.1 N HCl when compared with that of unmilled pure aceclofenac. These results were further supported by in vitro release studies of nanocrystals where an appreciable dissolution velocity with 100.07%±2.38% release was observed for aceclofenac nanocrystals compared with 47.66%±4.53% release for pure unmilled aceclofenac at the end of 2 h. The in vivo pharmacokinetic data generated showed a statistically significant increase in the C max for aceclofenac nanocrystals of 3.75±0.28 µg/mL (for pure unmilled aceclofenac C max was 1.96±0.17 µg/mL). The results obtained indicated that the developed nanocrystals of aceclofenac were successful in improving the solubility, thus the absorption and bioavailability of the drug. Hence, it may be a viable and cost-effective alternative to the current therapy.

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Recent developments in the use of nanocrystals to improve bioavailability of APIs

Ding,

Zhao,

Fang

et al. 2024

WIREs Nanomed Nanobiotechnol

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Nanocrystals refer to materials with at least one dimension smaller than 100 nm, composing of atoms arranged in single crystals or polycrystals. Nanocrystals have significant research value as they offer unique advantages over conventional pharmaceutical formulations, such as high bioavailability, enhanced targeting selectivity and controlled release ability and are therefore suitable for the delivery of a wide range of drugs such as insoluble drugs, antitumor drugs and genetic drugs with broad application prospects. In recent years, research on nanocrystals has been progressively refined and new products have been launched or entered the clinical phase of studies. However, issues such as safety and stability still stand that need to be addressed for further development of nanocrystal formulations, and significant gaps do exist in research in various fields in this pharmaceutical arena. This paper presents a systematic overview of the advanced development of nanocrystals, ranging from the preparation approaches of nanocrystals with which the bioavailability of poorly water‐soluble drugs is improved, critical properties of nanocrystals and associated characterization techniques, the recent development of nanocrystals with different administration routes, the advantages and associated limitations of nanocrystal formulations, the mechanisms of physical instability, and the enhanced dissolution performance, to the future perspectives, with a final view to shed more light on the future development of nanocrystals as a means of optimizing the bioavailability of drug candidates.This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies Nanotechnology Approaches to Biology > Nanoscale Systems in Biology

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Development and evaluation of decorated aceclofenac nanocrystals

Cited by 30 publications

References 28 publications

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

A top-down technique to improve the solubility and bioavailability of aceclofenac: in vitro and in vivo studies

Recent developments in the use of nanocrystals to improve bioavailability of APIs

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