Special Issue "Lipid-Based Dosage Form"

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

Deadline for manuscript submissions: closed (31 May 2018)

Special Issue Editors

Guest Editor
Prof. Dr. Paul W S Heng

Department of Pharmacy, National University of Singapore, 21 Lower Kent Ridge Rd, Singapore 119077
Website | E-Mail
Interests: melt manufacturing processes; melt extrusion; melt encapsulation; lipoid-based dosage forms; spray congealing; lipid encapsulation; lipid formulations; lipid particulate systems
Guest Editor
Prof. Dr. Yishen Zhu

Pharmaceutical Engineering Department, Nanjing Technology University, Nanjing 210028, China
E-Mail
Interests: pharmaceutical technology, with emphasis in manufacturing processes and dosage form design

Special Issue Information

Dear Colleagues,

Excipients based on lipoid materials have attracted considerable interest in the design of dosage forms. Lipids are often low-melting-point materials and poorly water-wettable too. Hence, they are amendable to several manufacturing technologies and are used in several types of dosage forms. This Special Issue hopes to present novel innovations in lipid-based dosage forms and applications involving lipids in manufacturing processes. Research on various technologies to produce lipid-based dosage forms are welcome.

We look forward to your submission for this Special Issue.

Best regards,

Prof. Dr. Paul W S Heng
Prof. Dr. Yishen Zhu
Guest Editors

Manuscript Submission Information

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Keywords

  • Lipid
  • Melt
  • Extrusion
  • Congeal
  • Non-aqueous
  • Controlled release
  • Taste masking
  • Encapsulation

Published Papers (4 papers)

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Research

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Open AccessArticle Effect of Lipid Additives and Drug on the Rheological Properties of Molten Paraffin Wax, Degree of Surface Drug Coating, and Drug Release in Spray-Congealed Microparticles
Pharmaceutics 2018, 10(3), 75; https://doi.org/10.3390/pharmaceutics10030075
Received: 4 June 2018 / Revised: 19 June 2018 / Accepted: 20 June 2018 / Published: 26 June 2018
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Abstract
Paraffin wax is potentially useful for producing spray-congealed drug-loaded microparticles with sustained-release and taste-masking properties. To date, there is little information about the effects of blending lipids with paraffin wax on the melt viscosity. In addition, drug particles may not be entirely coated
[...] Read more.
Paraffin wax is potentially useful for producing spray-congealed drug-loaded microparticles with sustained-release and taste-masking properties. To date, there is little information about the effects of blending lipids with paraffin wax on the melt viscosity. In addition, drug particles may not be entirely coated by the paraffin wax matrix. In this study, drug-loaded paraffin wax microparticles were produced by spray-congealing, and the effects of lipid additives on the microparticle production were investigated. The influence of lipid additives (stearic acid, cetyl alcohol, or cetyl esters) and drug (paracetamol) on the rheological properties of paraffin wax were elucidated. Fourier transform-infrared spectroscopy was conducted to investigate the interactions between the blend constituents. Selected formulations were spray-congealed, and the microparticles produced were characterized for their size, drug content, degree of surface drug coating, and drug release. The viscosity of wax-lipid blends was found to be mostly lower than the weighted viscosity when interactions occurred between the blend constituents. Molten paraffin wax exhibited Newtonian flow, which was transformed to plastic flow by paracetamol and pseudoplastic flow by the lipid additive. The viscosity was decreased with lipid added. Compared to plain wax, wax-lipid blends produced smaller spray-congealed microparticles. Drug content remained high. Degree of surface drug coating and drug release were also higher. The lipid additives altered the rheological properties and hydrophobicity of the melt and are useful for modifying the microparticle properties. Full article
(This article belongs to the Special Issue Lipid-Based Dosage Form)
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Open AccessArticle Design, Optimization and Characterization of a Transfersomal Gel Using Miconazole Nitrate for the Treatment of Candida Skin Infections
Pharmaceutics 2018, 10(1), 26; https://doi.org/10.3390/pharmaceutics10010026
Received: 19 January 2018 / Revised: 17 February 2018 / Accepted: 20 February 2018 / Published: 23 February 2018
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Abstract
Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrier function of the skin. MIC Transfersomes
[...] Read more.
Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrier function of the skin. MIC Transfersomes were prepared using a thin lipid film hydration technique. The prepared Transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC Transfersomes was incorporated into a Carbapol 934 gel base which was evaluated in comparison with a marketed product (Daktarin® cream 2%) for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro and in vivo antifungal activity. The prepared MIC Transfersomes had a high EE% ranging from (67.98 ± 0.66%) to (91.47 ± 1.85%), with small particle sizes ranging from (63.5 ± 0.604 nm) to (84.5 ± 0.684 nm). The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. The kinetic analysis of all release profiles was found to follow Higuchi’s diffusion model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). The prepared MIC transfersomal gel showed higher antifungal activity than Daktarin® cream 2%. Therefore, miconazole nitrate in the form of Transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier. Full article
(This article belongs to the Special Issue Lipid-Based Dosage Form)
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Review

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Open AccessFeature PaperReview Impact of Particle Size and Polydispersity Index on the Clinical Applications of Lipidic Nanocarrier Systems
Pharmaceutics 2018, 10(2), 57; https://doi.org/10.3390/pharmaceutics10020057
Received: 14 April 2018 / Revised: 15 May 2018 / Accepted: 17 May 2018 / Published: 18 May 2018
Cited by 1 | PDF Full-text (2827 KB) | HTML Full-text | XML Full-text
Abstract
Lipid-based drug delivery systems, or lipidic carriers, are being extensively employed to enhance the bioavailability of poorly-soluble drugs. They have the ability to incorporate both lipophilic and hydrophilic molecules and protecting them against degradation in vitro and in vivo. There is a number
[...] Read more.
Lipid-based drug delivery systems, or lipidic carriers, are being extensively employed to enhance the bioavailability of poorly-soluble drugs. They have the ability to incorporate both lipophilic and hydrophilic molecules and protecting them against degradation in vitro and in vivo. There is a number of physical attributes of lipid-based nanocarriers that determine their safety, stability, efficacy, as well as their in vitro and in vivo behaviour. These include average particle size/diameter and the polydispersity index (PDI), which is an indication of their quality with respect to the size distribution. The suitability of nanocarrier formulations for a particular route of drug administration depends on their average diameter, PDI and size stability, among other parameters. Controlling and validating these parameters are of key importance for the effective clinical applications of nanocarrier formulations. This review highlights the significance of size and PDI in the successful design, formulation and development of nanosystems for pharmaceutical, nutraceutical and other applications. Liposomes, nanoliposomes, vesicular phospholipid gels, solid lipid nanoparticles, transfersomes and tocosomes are presented as frequently-used lipidic drug carriers. The advantages and limitations of a range of available analytical techniques used to characterize lipidic nanocarrier formulations are also covered. Full article
(This article belongs to the Special Issue Lipid-Based Dosage Form)
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Open AccessReview Molecular Targeting of Acid Ceramidase in Glioblastoma: A Review of Its Role, Potential Treatment, and Challenges
Pharmaceutics 2018, 10(2), 45; https://doi.org/10.3390/pharmaceutics10020045
Received: 5 March 2018 / Revised: 3 April 2018 / Accepted: 4 April 2018 / Published: 9 April 2018
Cited by 1 | PDF Full-text (1105 KB) | HTML Full-text | XML Full-text
Abstract
Glioblastoma is the most common, malignant primary tumor of the central nervous system. The average prognosis for life expectancy after diagnosis, with the triad of surgery, chemotherapy, and radiation therapy, is less than 1.5 years. Chemotherapy treatment is mostly limited to temozolomide. In
[...] Read more.
Glioblastoma is the most common, malignant primary tumor of the central nervous system. The average prognosis for life expectancy after diagnosis, with the triad of surgery, chemotherapy, and radiation therapy, is less than 1.5 years. Chemotherapy treatment is mostly limited to temozolomide. In this paper, the authors review an emerging, novel drug called acid ceramidase, which targets glioblastoma. Its role in cancer treatment in general, and more specifically, in the treatment of glioblastoma, are discussed. In addition, the authors provide insights on acid ceramidase as a potential druggable target for glioblastoma. Full article
(This article belongs to the Special Issue Lipid-Based Dosage Form)
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