Microarrays and microneedle arrays for delivery of peptides, proteins, vaccines and other applications.
ABSTRACT Introduction: Peptide and protein microarray and microneedle array technology provides direct information on protein function and potential drug targets in drug discovery and delivery. Because of this unique ability, these arrays are well suited for protein profiling, drug target identification/validation and studies of protein interaction, biochemical activity, immune responses, clinical prognosis and diagnosis and for gene, protein and drug delivery. Areas covered: The aim of this review is to describe and summarize past and recent developments of microarrays in their construction, characterization and production and applications of microneedles in drug delivery. The scope and limitations of various technologies in this respect are discussed. Expert opinion: This article offers a review of microarray/microneedle technologies and possible future directions in targeting and in the delivery of pharmacologically active compounds for unmet needs in biopharmaceutical research. A better understanding of the production and use of microarrays and microneedles for delivery of peptides, proteins and vaccines is needed.
SourceAvailable from: Ryan F Donnelly[Show abstract] [Hide abstract]
ABSTRACT: We describe, for the first time, hydrogel-forming microneedle arrays prepared from "super swelling" polymeric compositions. We produced a microneedle formulation with enhanced swelling capabilities from aqueous blends containing 20% w/w Gantrez S-97, 7.5% w/w PEG 10,000 and 3% w/w Na2CO3 and utilised a drug reservoir of a lyophilised wafer-like design. These microneedle-lyophilised wafer compositions were robust and effectively penetrated skin, swelling extensively, but being removed intact. In in vitro delivery experiments across excised neonatal porcine skin, approximately 44 mg of the model high dose small molecule drug ibuprofen sodium was delivered in 24 h, equating to 37% of the loading in the lyophilised reservoir. The super swelling microneedles delivered approximately 1.24 mg of the model protein ovalbumin over 24 h, equivalent to a delivery efficiency of approximately 49%. The integrated microneedle-lyophilised wafer delivery system produced a progressive increase in plasma concentrations of ibuprofen sodium in rats over 6 h, with a maximal concentration of approximately 179 µg/ml achieved in this time. The plasma concentration had fallen to 71±6.7 µg/ml by 24 h. Ovalbumin levels peaked in rat plasma after only 1 hour at 42.36±17.01 ng/ml. Ovalbumin plasma levels then remained almost constant up to 6 h, dropping somewhat at 24 h, when 23.61±4.84 ng/ml was detected. This work represents a significant advancement on conventional microneedle systems, which are presently only suitable for bolus delivery of very potent drugs and vaccines. Once fully developed, such technology may greatly expand the range of drugs that can be delivered transdermally, to the benefit of patients and industry. Accordingly, we are currently progressing towards clinical evaluations with a range of candidate molecules.PLoS ONE 10/2014; 9(10):e111547. DOI:10.1371/journal.pone.0111547 · 3.53 Impact Factor
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ABSTRACT: Figure optionsDownload full-size imageDownload high-quality image (403 K)Download as PowerPoint slideInternational Journal of Pharmaceutics 01/2014; · 3.79 Impact Factor
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ABSTRACT: Aim: This study aimed to investigate transdermal delivery of proteins using combination of microporation and iontophoresis (ITP). Materials & methods & results: Delivery of model protein, Alexa Fluor 555 bovine serum albumin conjugate (AF-BSA) using ITP alone, microneedle (MN) alone, and ITP plus MN combination was assessed using confocal microscopy. Compared to MN alone, combination of MN plus ITP significantly increased skin's penetration depth of AF-BSA (300 vs 110 μm) and achieved lateral distribution of the model protein. Average fluorescence intensity quantified around each microchannel was 23.7-fold (8.2-fold, in vivo) higher for combination treatment compared with MN alone, in vitro. After 1 h in vitro permeation study, the unlabeled BSA amount delivered across skin was found to be 0, 1.4, 0.63 and 14 μg by passive, MN alone, ITP alone and ITP plus MN combination delivery, respectively.Therapeutic delivery 05/2014; 5(5):525-36. DOI:10.4155/tde.14.19