Special Issue "Nanocrystals"

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (15 March 2016)

Special Issue Editors

Guest Editor
Dr. Leena Peltonen

Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, Finland
Website | E-Mail
Interests: nanocrystals; nanoparticles; dissolution; solubility; physicochemical characterization
Guest Editor
Prof. Dr. Arvind K. Bansal

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar (Mohali), Punjab 160 062, India
Website | E-Mail
Phone: +91-0172-2214 682 (Ext. 2126)
Fax: +91-172-2214692
Interests: pre-formulation profiling; solid state characterization; polymorphism; amorphous systems; particle engineering; nano-crystalline dispersions; enhancement of oral bioavailability

Special Issue Information

Dear Colleagues:

Studies related to pharmaceutical nanocrystal started in the beginning of 1990’s and first product entered the market after 10 years of intensive research. Today, the number of marketed products is increasing all the time. Products for different drug delivery routes and various categories of dosage forms like oral solids and liquids have been marketed. The first applications nanocrystals were for improved solubility, and this is still the most well-known property of nanocrystal formulations. However, novel applications like controlled release formulations are also being studied. Accordingly, nanocrystals can be said to be very versatile option for drug delivery purposes.

This Special Issue on nanocrystals will include a variety of research articles, both reviews and original research contributions, dealing with drug nanocrystals. This special issue of Pharmaceutics, aims to provide an overview of well established nanocrystal technologies, marketed products and emerging areas for application of nanocrystals. We invite manuscripts dealing with topics related to development, manufacturing, quality and in vivo fate of nanocrystals.

Dr. Leena Peltonen
Dr. Arvind Bansal
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access quarterly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • nanocrystals
  • solubility
  • dissolution
  • controlled release
  • formulation
  • nanotechnology

Published Papers (5 papers)

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Research

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Open AccessArticle TPGS-Stabilized Curcumin Nanoparticles Exhibit Superior Effect on Carrageenan-Induced Inflammation in Wistar Rat
Pharmaceutics 2016, 8(3), 24; https://doi.org/10.3390/pharmaceutics8030024
Received: 4 June 2016 / Revised: 26 July 2016 / Accepted: 8 August 2016 / Published: 16 August 2016
Cited by 3 | PDF Full-text (5766 KB) | HTML Full-text | XML Full-text
Abstract
Curcumin, a hydrophobic polyphenol compound derived from the rhizome of the Curcuma genus, has a wide spectrum of biological and pharmacological applications. Previously, curcumin nanoparticles with different stabilizers had been produced successfully in order to enhance solubility and per oral absorption. In the
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Curcumin, a hydrophobic polyphenol compound derived from the rhizome of the Curcuma genus, has a wide spectrum of biological and pharmacological applications. Previously, curcumin nanoparticles with different stabilizers had been produced successfully in order to enhance solubility and per oral absorption. In the present study, we tested the anti-inflammatory effect of d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS)-stabilized curcumin nanoparticles in vivo. Lambda-carrageenan (λ-carrageenan) was used to induce inflammation in rats; it was given by an intraplantar route and intrapelurally through surgery in the pleurisy test. In the λ-carrageenan-induced edema model, TPGS-stabilized curcumin nanoparticles were given orally one hour before induction and at 0.5, 4.5, and 8.5 h after induction with two different doses (1.8 and 0.9 mg/kg body weight (BW)). Sodium diclofenac with a dose of 4.5 mg/kg BW was used as a standard drug. A physical mixture of curcumin-TPGS was also used as a comparison with a higher dose of 60 mg/kg BW. The anti-inflammatory effect was assessed on the edema in the carrageenan-induced paw edema model and by the volume of exudate as well as the number of leukocytes reduced in the pleurisy test. TPGS-stabilized curcumin nanoparticles with lower doses showed better anti-inflammatory effects, indicating the greater absorption capability through the gastrointestinal tract. Full article
(This article belongs to the Special Issue Nanocrystals)
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Open AccessFeature PaperCommunication Turning Waste into Value: Nanosized Natural Plant Materials of Solanum incanum L. and Pterocarpus erinaceus Poir with Promising Antimicrobial Activities
Pharmaceutics 2016, 8(2), 11; https://doi.org/10.3390/pharmaceutics8020011
Received: 2 February 2016 / Revised: 20 March 2016 / Accepted: 23 March 2016 / Published: 19 April 2016
Cited by 8 | PDF Full-text (7354 KB) | HTML Full-text | XML Full-text
Abstract
Numerous plants are known to exhibit considerable biological activities in the fields of medicine and agriculture, yet access to their active ingredients is often complicated, cumbersome and expensive. As a consequence, many plants harbouring potential drugs or green phyto-protectants go largely unnoticed, especially
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Numerous plants are known to exhibit considerable biological activities in the fields of medicine and agriculture, yet access to their active ingredients is often complicated, cumbersome and expensive. As a consequence, many plants harbouring potential drugs or green phyto-protectants go largely unnoticed, especially in poorer countries which, at the same time, are in desperate need of antimicrobial agents. As in the case of plants such as the Jericho tomato, Solanum incanum, and the common African tree Pterocarpus erinaceus, nanosizing of original plant materials may provide an interesting alternative to extensive extraction and isolation procedures. Indeed, it is straightforward to obtain considerable amounts of such common, often weed-like plants, and to mill the dried material to more or less uniform particles of microscopic and nanoscopic size. These particles exhibit activity against Steinernema feltiae or Escherichia coli, which is comparable to the ones seen for processed extracts of the same, respective plants. As S. feltiae is used as a model nematode indicative of possible phyto-protective uses in the agricultural arena, these findings also showcase the potential of nanosizing of crude “waste” plant materials for specific practical applications, especially—but not exclusively—in developing countries lacking a more sophisticated industrial infrastructure. Full article
(This article belongs to the Special Issue Nanocrystals)
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Review

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Open AccessReview Performance Parameters and Characterizations of Nanocrystals: A Brief Review
Pharmaceutics 2016, 8(3), 26; https://doi.org/10.3390/pharmaceutics8030026
Received: 1 April 2016 / Revised: 22 June 2016 / Accepted: 22 August 2016 / Published: 30 August 2016
Cited by 8 | PDF Full-text (820 KB) | HTML Full-text | XML Full-text
Abstract
Poor bioavailability of drugs associated with their poor solubility limits the clinical effectiveness of almost 40% of the newly discovered drug moieties. Low solubility, coupled with a high log p value, high melting point and high dose necessitates exploration of alternative formulation strategies
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Poor bioavailability of drugs associated with their poor solubility limits the clinical effectiveness of almost 40% of the newly discovered drug moieties. Low solubility, coupled with a high log p value, high melting point and high dose necessitates exploration of alternative formulation strategies for such drugs. One such novel approach is formulation of the drugs as “Nanocrystals”. Nanocrystals are primarily comprised of drug and surfactants/stabilizers and are manufactured by “top-down” or “bottom-up” methods. Nanocrystals aid the clinical efficacy of drugs by various means such as enhancement of bioavailability, lowering of dose requirement, and facilitating sustained release of the drug. This effect is dependent on the various characteristics of nanocrystals (particle size, saturation solubility, dissolution velocity), which have an impact on the improved performance of the nanocrystals. Various sophisticated techniques have been developed to evaluate these characteristics. This article describes in detail the various characterization techniques along with a brief review of the significance of the various parameters on the performance of nanocrystals. Full article
(This article belongs to the Special Issue Nanocrystals)
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Open AccessReview Nanomilling of Drugs for Bioavailability Enhancement: A Holistic Formulation-Process Perspective
Pharmaceutics 2016, 8(2), 17; https://doi.org/10.3390/pharmaceutics8020017
Received: 15 March 2016 / Revised: 13 May 2016 / Accepted: 13 May 2016 / Published: 20 May 2016
Cited by 22 | PDF Full-text (1588 KB) | HTML Full-text | XML Full-text
Abstract
Preparation of drug nanoparticles via wet media milling (nanomilling) is a very versatile drug delivery platform and is suitable for oral, injectable, inhalable, and buccal applications. Wet media milling followed by various drying processes has become a well-established and proven formulation approach especially
[...] Read more.
Preparation of drug nanoparticles via wet media milling (nanomilling) is a very versatile drug delivery platform and is suitable for oral, injectable, inhalable, and buccal applications. Wet media milling followed by various drying processes has become a well-established and proven formulation approach especially for bioavailability enhancement of poorly water-soluble drugs. It has several advantages such as organic solvent-free processing, tunable and relatively high drug loading, and applicability to a multitude of poorly water-soluble drugs. Although the physical stability of the wet-milled suspensions (nanosuspensions) has attracted a lot of attention, fundamental understanding of the process has been lacking until recently. The objective of this review paper is to present fundamental insights from available published literature while summarizing the recent advances and highlighting the gap areas that have not received adequate attention. First, stabilization by conventionally used polymers/surfactants and novel stabilizers is reviewed. Then, a fundamental understanding of the process parameters, with a focus on wet stirred media milling, is revealed based on microhydrodynamic models. This review is expected to bring a holistic formulation-process perspective to the nanomilling process and pave the way for robust process development scale-up. Finally, challenges are indicated with a view to shedding light on future opportunities. Full article
(This article belongs to the Special Issue Nanocrystals)
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Open AccessReview Stabilizing Agents for Drug Nanocrystals: Effect on Bioavailability
Pharmaceutics 2016, 8(2), 16; https://doi.org/10.3390/pharmaceutics8020016
Received: 15 March 2016 / Revised: 12 May 2016 / Accepted: 16 May 2016 / Published: 20 May 2016
Cited by 16 | PDF Full-text (2673 KB) | HTML Full-text | XML Full-text
Abstract
Drug nanocrystals are a versatile option for drug delivery purposes, and while the number of poorly soluble drug materials is all the time increasing, more research in this area is performed. Drug nanocrystals have a simple structure—a solid drug core is surrounded by
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Drug nanocrystals are a versatile option for drug delivery purposes, and while the number of poorly soluble drug materials is all the time increasing, more research in this area is performed. Drug nanocrystals have a simple structure—a solid drug core is surrounded by a layer of stabilizing agent. However, despite the considerably simple structure, the selection of an appropriate stabilizer for a certain drug can be challenging. Mostly, the stabilizer selection is based purely on the requirement of physical stability, e.g., maintaining the nanosized particle size as long as possible after the formation of drug nanocrystals. However, it is also worth taking into account that stabilizer can affect the bioavailability in the final formulation via interactions with cells and cell layers. In addition, formation of nanocrystals is only one process step, and for the final formulation, more excipients are often added to the composition. The role of the stabilizers in the final formulation can be more than only stabilizing the nanocrystal particle size. A good example is the stabilizer’s role as cryoprotectant during freeze drying. In this review, the stabilizing effect, role of stabilizers in final nanocrystalline formulations, challenges in reaching in vitro–in vivo correlation with nanocrystalline products, and stabilizers’ effect on higher bioavailability are discussed. Full article
(This article belongs to the Special Issue Nanocrystals)
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