Hydrophilic Matrices for Oral Control Drug Delivery

Oral controlled drug delivery has gathered tremendous attention over the years due to its many advantages over conventional dosage forms. Polymer-based matrices have become an integral part of the pharmaceutical industry. Hydrophilic matrices are capable of controlling the release of drug over an extended period of time. Hydrophilic polymers, especially the hydrophilic derivatives of cellulose ethers, are frequently used for these applications. Therefore, the objective of this review is to discuss the scientific and physicochemical aspects of these polymeric systems that can affect the drug release from such formulation

Solid Lipid Nanoparticles: A Potential Approach for Dermal Drug Delivery

Solid lipid nanoparticles (SLNs) have attracted increasing attention during recent years. Due to their unique size dependent properties, lipid nanoparticles offer possibilities to develop new therapeutics. The ability to incorporate drugs into nanoparticles offers a new prototype in drug delivery thus realizing the dual goal of both controlled release and site-specific drug delivery. Drug delivery to the skin is widely used for local and systemic delivery and has potential to be improved by application of nanoparticulate formulations. If investigated appropriately, solid lipid nanoparticles may open new opportunities in therapy of complex diseases which is difficult to treat

Tribo-electric Charging and Adhesion of Cellulose Ethers and their Mixtures with Flurbiprofen

The pervasiveness of tribo-electric charge during pharmaceutical processing can lead to the exacerbation of a range of problems including segregation, content heterogeneity and particle surface adhesion. The excipients, hydroxypropyl methylcellulose and methylcellulose, are often used in drug delivery systems and so it is important to understand the impact of associated factors on their charging and adhesion mechanisms, however, little work has been done. Such phenomena become more prominent when excipients are introduced to a powder mixture alongside the active pharmaceutical ingredient(s) (APIs) with inter- and intra-particulate interactions giving rise to electrification and surface adhesion of powder particles. The aim of this study was to understand the impact of material attributes (particle size, hydroxypropyl (Hpo) to methoxyl (Meo) ratio and molecular size) on the charging and adhesion characteristics of cellulose ethers. Furthermore, poorly compactible and highly electrostatically charged drug, flurbiprofen, was used to develop binary powder mixtures having different polymer to drug levels. Subsequently, a relationship between tribo-electric charging and surface adhesion was studied. Charge was induced on powder particles and measured using a custom built device based on a shaking concept consisting of a Faraday cup connected to electrometer. The diversity in physicochemical properties has shown a significant impact on the tribo-electric charging and adhesion behaviour of MC and HPMC. Moreover, the adhesion and electrostatic charge of the API was significantly reduced when MC and HPMC were incorporated. Moreover, tribo-electric charging shows a linear relationship (R2= 0.81-0.98) with particle surface adhesion, however, other factors were also involved. It is anticipated that such reduction in charge and particle surface adhesion would improve flow and compaction properties during processing

The influence of fillers on theophylline release from clay matrices

Abstract: The objectives of this study were to investigate the suitability of magnesium aluminium silicate (MAS) (Veegum®) to control drug release of a model drug, theophylline, from tablet matrices. To this end, the performance of three commonly used fillers namely: lactose, microcrystalline cellulose (Avicel PH102; MCC), and pre-gelatinized starch, Starch 1500 PGS), were evaluated against Veegum®. The physico-mechanical properties of the tablet matrices were studied along with dissolution studies to determine the effect of single or binary mixtures of the excipients on the drug release pattern. A DSC hydration methodology was also employed to characterize the states of water present in the tablet matrices and to determine any impact on drug release. Formulations containing MAS alone produced compacts with the lowest hardness (4.5 kp) whereas formulations containing MCC alone produced the hardest tablets (17.2 kp). Dissolution studies suggested that matrices containing MAS alone released the theophylline quickest as compared to lactose, MCC or PGS. It was difficult to establish a trend of the bound and free water states in the tablet matrices; however the formulation containing only MAS had the highest bound water at 29 %. The results therefore show that theophylline does not interact with MAS. As such the dominant factor in controlling drug release using MAS requires interaction or intercalation with a cationic drug. In the absence of this however, other excipients can play a role in controlling drug release. Keywords: Veegum, clay matrices, DSC hydration, Magnesium aluminium silicate, filler

The delivery of bioactive proteins using biodegradable microspheres

In this project, antigen-containing microspheres were produced using a range of biodegradable polymers by single and double emulsion solvent evaporation and spray drying techniques. The proteins used in this study were mainly BSA, tetanus toxoid, F1 and V, Y. pestis subunit vaccines and the cytokine, interferon-gamma. The polymer chosen for use in the vaccine preparation will directly determine the characteristics of the formulation. Full in vitro analysis of the preparations was carried out, including surface hydrophobicity and drug release profiles. The influence of the surfactants employed on microsphere surface hydrophobicity was demonstrated. Preparations produced with polyhydroxybutyrate and poly(DTH carbonate) polymers were also shown to be more hydrophobic than PLA microspheres, which may enhance particle uptake by antigen presenting cells and Peyer's patches. Systematic immunisation with microspheres with a range of properties showed differences in the time course and extent of the immune response generated, which would allow optimisation of the dosing schedule to provide maximal response in a single dose preparation. Both systematic and mucosal responses were induced following oral delivery of microencapsulated tetanus toxoid indicating that the encapsulation of the antigen into a microsphere preparation provides protection in the gut and allows targeting of the mucosal-associated lymphoid tissue. Co-encapsulation of adjuvants for further enhancement of immune response was also carried out and the effect on loading and release pattern assessed. Co-encapsulated F1 and interferon-gamma was administered i.p. and the immune responses compared with singly encapsulated and free subunit antigen

Editorial: maintaining open access to high quality publications at no cost to authors

The inability to access scientific literature freely can be a major obstacle in the advancement of science. Many reputable journals offering optional open access incur a substantial upfront payment to cover their publication costs, and hence many authors cannot afford to publish open access papers in a journal with an established reputation. Publishers charging for article processing claim that the charge is necessary to maintain their reputation and costs for peer review, editing and indexing articles. Thus, some open-access publications have a less rigorous peer-review and editorial process

Nasal Drug Delivery Systems: An Overview

Since ancient times, drugs have been administered via the nasal route for therapeutic and recreational purposes. The interest in, and importance, of the systemic effects of drugs administered through the nasal route, have expanded over recent decades. Intra-nasal administration of drugs offers an interesting alternative for achieving systemic therapeutic effects of drugs that are comparable to the parenteral route, which can be inconvenient at times or oral administration, which can result in unacceptably low drug bioavailability. So, it is important to understand the potential and limitations of various nasal drug delivery systems. Therefore, the aim of this review article is to discuss the various pharmaceutical dosage forms that have the potential to be utilised for local or systemic drug administration. It is intuitively expected that this review will help to understand and further to develop suitable intra-nasal formulations to achieve specific therapeutic objectives