Bottom-up approaches for preparing drug nanocrystals: Formulations and factors affecting particle size

Sinha, Biswadip; Müller, Rainer H.; Möschwitzer, Jan P.

doi:10.1016/j.ijpharm.2013.01.019

Cited by 416 publications

(338 citation statements)

References 169 publications

Supporting

Mentioning

327

Contrasting

Unclassified

Order By: Relevance

“…183 The top-down method starts from large crystals to small NCs in a step-by-step manner during a high-energy process, such as pearl milling and high-pressure homogenization. 182,[184][185][186] The bottom-up method involves procedures that start from molecules to NCs, such as solvent exchange, 21,[187][188][189] high-gravity-control precipitation, 188,190,191 evaporative precipitation, 192 rapid expansion of supercritical solution, 193 and supercritical antisolvent methods. 194 DNCs prepared via bottom-up methods need less energy and are smaller compared with those prepared through top-down methods.…”

Section: Drug Nanocrystalsmentioning

confidence: 99%

High drug-loading nanomedicines: progress, current status, and prospects

Shen

Liu

et al. 2017

IJN

413

268

View full text Add to dashboard Cite

Drug molecules transformed into nanoparticles or endowed with nanostructures with or without the aid of carrier materials are referred to as “nanomedicines” and can overcome some inherent drawbacks of free drugs, such as poor water solubility, high drug dosage, and short drug half-life in vivo. However, most of the existing nanomedicines possess the drawback of low drug-loading (generally less than 10%) associated with more carrier materials. For intravenous administration, the extensive use of carrier materials might cause systemic toxicity and impose an extra burden of degradation, metabolism, and excretion of the materials for patients. Therefore, on the premise of guaranteeing therapeutic effect and function, reducing or avoiding the use of carrier materials is a promising alternative approach to solve these problems. Recently, high drug-loading nanomedicines, which have a drug-loading content higher than 10%, are attracting increasing interest. According to the fabrication strategies of nanomedicines, high drug-loading nanomedicines are divided into four main classes: nanomedicines with inert porous material as carrier, nanomedicines with drug as part of carrier, carrier-free nanomedicines, and nanomedicines following niche and complex strategies. To date, most of the existing high drug-loading nanomedicines belong to the first class, and few research studies have focused on other classes. In this review, we investigate the research status of high drug-loading nanomedicines and discuss the features of their fabrication strategies and optimum proposal in detail. We also point out deficiencies and developing direction of high drug-loading nanomedicines. We envision that high drug-loading nanomedicines will occupy an important position in the field of drug-delivery systems, and hope that novel perspectives will be proposed for the development of high drug-loading nanomedicines.

show abstract

Section: Drug Nanocrystalsmentioning

confidence: 99%

High drug-loading nanomedicines: progress, current status, and prospects

Shen

Liu

et al. 2017

IJN

413

268

View full text Add to dashboard Cite

show abstract

“…The current demand for micro/nano-material various applications in medical and pharmaceutical industry especially in drug delivery has triggered the research in organic crystal engineering and development (3,4). Crystal engineering is particularly important for the development of pharmaceutical molecules in the context of improved drug delivery or bio-labelling/bio-sensing (5,6).…”

Section: Introductionmentioning

confidence: 99%

RETRACTED ARTICLE: Study of the Transformations of Micro/Nano-crystalline Acetaminophen Polymorphs in Drug-Polymer Binary Mixtures

et al. 2016

View full text Add to dashboard Cite

Abstract.This study elucidates the physical properties of sono-crystallised micro/nano-sized acetaminophen/paracetamol (PMOL) and monitors its possible transformation from polymorphic form I (monoclinic) to form II (orthorhombic). Hydrophilic Plasdone® S630 copovidone (S630), N-vinyl-2-pyrrolidone and vinyl acetate copolymer, and methacrylate-based cationic copolymer, Eudragit® EPO (EPO), were used as polymeric carriers to prepare drug/polymer binary mixtures. Commercially available PMOL was crystallised under ultra sound sonication to produce micro/nano-sized (0.2-10 microns) crystals in monoclinic form. Homogeneous binary blends of drug-polymer mixtures at various drug concentrations were obtained via a thorough mixing. The analysis conducted via the single X-ray crystallography determined the detailed structure of the crystallised PMOL in its monoclinic form. The solid state and the morphology analyses of the PMOL in the binary blends evaluated via differential scanning calorimetry (DSC), modulated temperature DSC (MTDSC), scanning electron microscopy (SEM) and hot stage microscopy (HSM) revealed the crystalline existence of the drug within the amorphous polymeric matrices. The application of temperature controlled X-ray diffraction (VTXRPD) to study the polymorphism of PMOL showed that the most stable form I (monoclinic) was altered to its less stable form II (orthorhombic) at high temperature (>112°C) in the binary blends regardless of the drug amount. Thus, VTXRD was used as a useful tool to monitor polymorphic transformations of crystalline drug (e.g. PMOL) to assess their thermal stability in terms of pharmaceutical product development and research.

show abstract

“…Stirring was continued for few minutes after the injection to yield smaller particles with narrow size distribution [52]. Nucleation occurs at the interphase between the droplets of the solution and the antisolvent (water).…”

Section: Resultsmentioning

confidence: 99%

“…But, a number of experimental factors such as temperature of the antisolvent, concentration of the solution, rate of injection, nozzle geometry, ratio of solvent to antisolvent and ultrasonication affect the particle size and morphology of the nanoparticles [52]. Most of the experimental parameters that are required for the formation of smaller particles were optimized in one of our previous studies [52]. The previously optimized experimental parameters were used in the present study as the solvent (acetone)-antisolvent (water) pair was the same.…”

Section: Resultsmentioning

confidence: 99%

Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs

Kumar

Siril

Javid

2016

Materials Science and Engineering: C

View full text Add to dashboard Cite

The non-steroidal anti-inflammatory drugs (NSAIDs) are the most widely used pharmaceuticals worldwide. Interestingly, many of them have significant anticancer properties too. However, the poor water solubility of certain NSAIDs limits their application for cancer treatment. Nanosizing of such drugs can help to improve the solubility and this may result in enhanced anticancer activities too. Moreover, over dosages and the accompanying side effects of NSAIDs can be minimized by improving their solubility and bioavailability. Successful nanoformulation of three NSAIDs: ibuprofen (IBP), ketoprufen (KP) and naproxen (NAP) using a novel evaporation assisted solvent-antisolvent interaction (EASAI) method is reported here. Three water soluble and biocompatible polymers: polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA) and hydroxypropyl methylcellulose (HPMC) were used to stabilize the drug nanoparticles. Particles having spherical morphology with average size below 30 nm were thoroughly characterized using dynamic light scattering and field emission scanning electron microscopy (FESEM) imaging. The nanoformulation resulted in ten to fifteen fold improvements in the solubility and significant enhancement in the in-vitro drug release profiles of the NSAIDs. Anticancer screening of the nanoformulated NSAIDs against five different cancer cell lines such as MCF-7 (Human breast cancer cell line), (Human pancreatic cancer cell line) MIA-PA-CA-2, (Human colon cancer cell line) HT-29, (Human leukemia cell line) Jurkat and (human ovarian carcinoma cell line) A2780 was performed. All the nanoformulated samples showed improved anticancer activity against the Leukemia cancer cell line, out of which NAP-PVP showed the highest anti-cancer activity. The anti-Leukemia activity of NAP-PVP was more than twice that of doxorubicin which is a standard anticancer drug.

show abstract

Bottom-up approaches for preparing drug nanocrystals: Formulations and factors affecting particle size

Cited by 416 publications

References 169 publications

High drug-loading nanomedicines: progress, current status, and prospects

High drug-loading nanomedicines: progress, current status, and prospects

RETRACTED ARTICLE: Study of the Transformations of Micro/Nano-crystalline Acetaminophen Polymorphs in Drug-Polymer Binary Mixtures

Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs

Contact Info

Product

Resources

About