Special Issue "Microencapsulation Technology Applied to Pharmaceutics"

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

Deadline for manuscript submissions: closed (31 August 2011).

Special Issue Editors

Prof. Dr. Denis Poncelet
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Guest Editor
Oniris, rue de la géraudière, BP 82225, 44322 Nantes, France
Interests: bioencapsulation; solid dispersion
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Thierry Vandamme
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Guest Editor
Laboratory for the Conception and Application of Bioactive Molecules, UMR 7199 CNRS, Faculty of Pharmacy, University of Strasbourg, France
Interests: the design and the formulation of drugs by using microencapsulation technologies; in vitro / in vivo drug release and mathematical modeling; controlled release of drugs from different raw materials allowing sustained release or targeting; application for different administration routes
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Microencapsulation is one of the techniques able to overcome the drug stability problem, and moreover, the possibility of formulating encapsulated drug delivery systems with controlled release rates. On these bases, microencapsulated dosage forms represent effective new therapeutic platforms. The active molecules are protected as long as they reach their specific action site. Most of the applied techniques of micro-encapsulation are based on modifications of the three basic methods: spray-drying, phase separation (coacervation), and solvent extraction/evaporation.

This special issue will cover the different interests of microencapsulation as a means to control or modify the release of drug substances from drug delivery systems. Since clinical efficacies have been reported to be improved by the encapsulation of pharmaceuticals, the bioavailability of drugs, control drug release kinetics, minimizing drug side effects, and taste masking of the bitter taste of drug substances will be discussed.

Prof. Dr. Thierry F. Vandamme
Prof. Dr. Denis Poncelet
Guest Editors

Keywords

  • microencapsulation
  • encapsulation
  • encapsulation efficiency
  • coacervation
  • entrapment
  • lipid formulation
  • water-in-oil emulsion
  • spray-congealing
  • emulsion solvent evaporation
  • membrane emulsification
  • size controlled emulsion
  • drug; targeting
  • microspheres
  • microparticles
  • microcapsules
  • coating
  • emulsion
  • polymeric drug delivery systems
  • spray-drying
  • taste masking
  • aerosol
  • electrospray
  • self microemulsifying

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Published Papers (8 papers)

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Research

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Article
Probiotic Encapsulation Technology: From Microencapsulation to Release into the Gut
Pharmaceutics 2012, 4(1), 149-163; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics4010149 - 06 Feb 2012
Cited by 121 | Viewed by 8315
Abstract
Probiotic encapsulation technology (PET) has the potential to protect microorgansisms and to deliver them into the gut. Because of the promising preclinical and clinical results, probiotics have been incorporated into a range of products. However, there are still many challenges to overcome with [...] Read more.
Probiotic encapsulation technology (PET) has the potential to protect microorgansisms and to deliver them into the gut. Because of the promising preclinical and clinical results, probiotics have been incorporated into a range of products. However, there are still many challenges to overcome with respect to the microencapsulation process and the conditions prevailing in the gut. This paper reviews the methodological approach of probiotics encapsulation including biomaterials selection, choice of appropriate technology, in vitro release studies of encapsulated probiotics, and highlights the challenges to be overcome in this area. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Article
Formulation Optimization of Sustained-Release Ammonio Methacrylate Copolymer Microspheres. Effects of Log P and Concentration of Polar Cosolvents, and Role of the Drug/Copolymer Ratio
Pharmaceutics 2011, 3(4), 830-847; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics3040830 - 10 Nov 2011
Cited by 4 | Viewed by 4856
Abstract
The objectives of this work were the formulation optimization of the preparation process parameters and to evaluate spray-dried sustained-release microspheres using ammonio methacrylate copolymer (AMC) as a polymer matrix. The effects of log P and the concentrations of the cosolvents (acetone, methyl ethyl [...] Read more.
The objectives of this work were the formulation optimization of the preparation process parameters and to evaluate spray-dried sustained-release microspheres using ammonio methacrylate copolymer (AMC) as a polymer matrix. The effects of log P and the concentrations of the cosolvents (acetone, methyl ethyl ketone and n-butyl acetate) and different drug/copolymer ratios as independent variables on the physicochemical parameters (the W1/O emulsion viscosity, the microsphere production yield, the average particle size, the encapsulation efficiency) and the cumulative in vitro drug release as dependent variables were studied. The optimization was carried out on the basis of the 33 factorial design study. The optimization process results showed that addition of polar cosolvents proved effective, linear relationships were observed between the independent and the dependent variables. The best conditions were achieved by microspheres prepared by using a low/medium cosolvent log P, cosolvent concentration of 25–50% v/v and a drug/copolymer ratio of 1:16. The microspheres ensured sustained release with Nernst and Baker-Lonsdale release profiles. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Article
Development of Re-Usable Yeast-Gellan Gum Micro-Bioreactors for Potential Application in Continuous Fermentation to Produce Bio-Ethanol
Pharmaceutics 2011, 3(4), 731-744; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics3040731 - 17 Oct 2011
Cited by 13 | Viewed by 5017
Abstract
The objectives of this study were to investigate the feasibility of encapsulating yeast cells using gellan gum by an emulsification method and to evaluate the fermentation efficiency and the reusability of the micro-bioreactors produced. It was found that yeast cells could be successfully [...] Read more.
The objectives of this study were to investigate the feasibility of encapsulating yeast cells using gellan gum by an emulsification method and to evaluate the fermentation efficiency and the reusability of the micro-bioreactors produced. It was found that yeast cells could be successfully encapsulated to form relatively spherical micro-bioreactors with high specific surface area for mass transfer. Cell viability was found to be reduced by one log reduction after the emulsification process. The ethanol yield of the micro-bioreactors was comparable to that of free yeast in the first fermentation cycle. The micro-bioreactors remained intact and could be re-used up to 10 cycles of fermentation. Despite cell breakthrough, relatively high ethanol yields were obtained, indicating that the micro-bioreactors also functioned as regenerative reservoirs of yeast. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Article
Effect of Microencapsulation Shear Stress on the Structural Integrity and Biological Activity of a Model Monoclonal Antibody, Trastuzumab
Pharmaceutics 2011, 3(3), 510-524; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics3030510 - 24 Aug 2011
Cited by 13 | Viewed by 4845
Abstract
The aim of the present study was to investigate the influence of process shear stressors on the stability of a model monoclonal antibody, trastuzumab. Trastuzumab, at concentrations of 0.4–4.0 mg/mL, was subjected to sonication, freeze-thaw, lyophilisation, spray drying and was encapsulated into micro- [...] Read more.
The aim of the present study was to investigate the influence of process shear stressors on the stability of a model monoclonal antibody, trastuzumab. Trastuzumab, at concentrations of 0.4–4.0 mg/mL, was subjected to sonication, freeze-thaw, lyophilisation, spray drying and was encapsulated into micro- and nanoparticles. The stressed samples were analysed for structural integrity by gel electrophoresis, SDS-PAGE, and size exclusion chromatography (SEC), while the conformational integrity was analysed by circular dichroism (CD). Biological activity of the stressed trastuzumab was investigated by measuring the inhibition of cell proliferation of HER-2 expressing cell lines. Results show that trastuzumab was resistant to the process shear stresses applied and to microencapsulation processes. At the lowest concentration of 0.4 mg/mL, a low percent ( 0.05). The results of this study conclude that trastuzumab may be resistant to various processing stresses. These findings have important implications with respect to pharmaceutical processing of monoclonal antibodies. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Review

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Review
Novel Experimental and Clinical Therapeutic Uses of Low-Molecular-Weight Heparin/Protamine Microparticles
Pharmaceutics 2012, 4(1), 42-57; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics4010042 - 11 Jan 2012
Cited by 9 | Viewed by 4527
Abstract
Low-molecular-weight heparin/protamine microparticles (LMW-H/P MPs) were produced as a carrier for heparin-binding growth factors (GFs) and for various adhesive cells. A mixture of low-molecular-weight heparin (MW: approximately 5000 Da, 6.4 mg/mL) and protamine (MW: approximately 3000 Da, 10 mg/mL) at a ratio of [...] Read more.
Low-molecular-weight heparin/protamine microparticles (LMW-H/P MPs) were produced as a carrier for heparin-binding growth factors (GFs) and for various adhesive cells. A mixture of low-molecular-weight heparin (MW: approximately 5000 Da, 6.4 mg/mL) and protamine (MW: approximately 3000 Da, 10 mg/mL) at a ratio of 7:3 (vol:vol) yields a dispersion of microparticles (0.5–3 µm in diameter). LMW-H/P MPs immobilize, control the release and protect the activity of GFs. LMW-H/P MPs can also bind to cell surfaces, causing these cells to interact with the LMW-H/P MPs, inducing cells/MPs-aggregate formation and substantially promoting cellular viability. Furthermore, LMW-H/P MPs can efficiently bind to tissue culture plates and retain the binding of important GFs, such as fibroblast growth factor (FGF)-2. The LMW-H/P MPs-coated matrix with various GFs or cytokines may provide novel biomaterials that can control cellular activity such as growth and differentiation. Thus, LMW-H/P MPs are an excellent carrier for GFs and various cells and are an efficient coating matrix for cell cultures. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Review
Trojan Microparticles for Drug Delivery
Pharmaceutics 2012, 4(1), 1-25; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics4010001 - 06 Jan 2012
Cited by 40 | Viewed by 5475
Abstract
During the last decade, the US Food and Drug Administration (FDA) have regulated a wide range of products, (foods, cosmetics, drugs, devices, veterinary, and tobacco) which may utilize micro and nanotechnology or contain nanomaterials. Nanotechnology allows scientists to create, explore, and manipulate materials [...] Read more.
During the last decade, the US Food and Drug Administration (FDA) have regulated a wide range of products, (foods, cosmetics, drugs, devices, veterinary, and tobacco) which may utilize micro and nanotechnology or contain nanomaterials. Nanotechnology allows scientists to create, explore, and manipulate materials in nano-regime. Such materials have chemical, physical, and biological properties that are quite different from their bulk counterparts. For pharmaceutical applications and in order to improve their administration (oral, pulmonary and dermal), the nanocarriers can be spread into microparticles. These supramolecular associations can also modulate the kinetic releases of drugs entrapped in the nanoparticles. Different strategies to produce these hybrid particles and to optimize the release kinetics of encapsulated drugs are discussed in this review. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Review
Encapsulation of Natural Polyphenolic Compounds; a Review
Pharmaceutics 2011, 3(4), 793-829; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics3040793 - 04 Nov 2011
Cited by 495 | Viewed by 14621
Abstract
Natural polyphenols are valuable compounds possessing scavenging properties towards radical oxygen species, and complexing properties towards proteins. These abilities make polyphenols interesting for the treatment of various diseases like inflammation or cancer, but also for anti-ageing purposes in cosmetic formulations, or for nutraceutical [...] Read more.
Natural polyphenols are valuable compounds possessing scavenging properties towards radical oxygen species, and complexing properties towards proteins. These abilities make polyphenols interesting for the treatment of various diseases like inflammation or cancer, but also for anti-ageing purposes in cosmetic formulations, or for nutraceutical applications. Unfortunately, these properties are also responsible for a lack in long-term stability, making these natural compounds very sensitive to light and heat. Moreover, polyphenols often present a poor biodisponibility mainly due to low water solubility. Lastly, many of these molecules possess a very astringent and bitter taste, which limits their use in food or in oral medications. To circumvent these drawbacks, delivery systems have been developed, and among them, encapsulation would appear to be a promising approach. Many encapsulation methods are described in the literature, among which some have been successfully applied to plant polyphenols. In this review, after a general presentation of the large chemical family of plant polyphenols and of their main chemical and biological properties, encapsulation processes applied to polyphenols are classified into physical, physico-chemical, chemical methods, and other connected stabilization methods. After a brief description of each encapsulation process, their applications to polyphenol encapsulation for pharmaceutical, food or cosmetological purposes are presented. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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Review
The Application of Microencapsulation Techniques in the Treatment of Endodontic and Periodontal Diseases
Pharmaceutics 2011, 3(3), 538-571; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics3030538 - 26 Aug 2011
Cited by 29 | Viewed by 6162
Abstract
In the treatment of intracanal and periodontal infections, the local application of antibiotics and other therapeutic agents in the root canal or in periodontal pockets may be a promising approach to achieve sustained drug release, high antimicrobial activity and low systemic side effects. [...] Read more.
In the treatment of intracanal and periodontal infections, the local application of antibiotics and other therapeutic agents in the root canal or in periodontal pockets may be a promising approach to achieve sustained drug release, high antimicrobial activity and low systemic side effects. Microparticles made from biodegradable polymers have been reported to be an effective means of delivering antibacterial drugs in endodontic and periodontal therapy. The aim of this review article is to assess recent therapeutic strategies in which biocompatible microparticles are used for effective management of periodontal and endodontic diseases. In vitro and in vivo studies that have investigated the biocompatibility or efficacy of certain microparticle formulations and devices are presented. Future directions in the application of microencapsulation techniques in endodontic and periodontal therapies are discussed. Full article
(This article belongs to the Special Issue Microencapsulation Technology Applied to Pharmaceutics)
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