Development of a skin-friendly microemulsion for dermal allergen-specific immunotherapy

Kiselmann, C.; Dobler, Dorota; Schmidts, Thomas; Eicher, Anna-Carola; Möbs, Christian; Pfützner, Wolfgang; Runkel, Frank

doi:10.1016/j.ijpharm.2018.09.002

Cited by 16 publications

(12 citation statements)

References 37 publications

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“…Microneedles (MN) have become an attractive platform to overcome the skin barrier for cutaneous drug delivery in an almost noninvasive manner (Henry et al,1998;Fakhraei et al, 2018;Kiselmann et al, 2018;Boopathy et al, 2019). MN are an array of needles miniaturized down to the micrometer scale.…”

Section: Introductionmentioning

confidence: 99%

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

et al. 2020

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Sinomenine (SIN) is an anti-inflammatory alkaloid derived from Sinomenium acutum, and the products sinomenine hydrochloride (SH) tablets and injections have been marketed in China to treat rheumatoid arthritis (RA). Oral administration of SH has shortcomings of gastrointestinal irritation and low bioavailability. The injection may require professional training and higher cost. It is of interest to develop an alternative form that is easier to administer and avoids the first-pass metabolism. In this study, SHloaded dissolving microneedles (SH-MN) were fabricated using polyvinyl pyrrolidone and chondroitin sulfate with a casting method. In percutaneous permeation studies of In vitro, the cumulative permeation and permeation rate of SH-MN were 5.31 and 5.06 times higher than that of SH-gel (SH-G). In percutaneous pharmacokinetic studies, the values of the area under the curve after administration of SH-MN in the skin and blood were 1.43-and 1.63-fold higher than that of SH-G, respectively. In percutaneous absorption studies, SH-MN could absorb into tissue fluid; and dissolve after skin penetration. The drug was released along the channel and spread to surrounding skin tissue. After 4 h, the needle tip was almost completely dissolved, and the drug could penetrate to a depth of 200 lm under the skin. These results demonstrate that the SH-MN is an effective, safe, and simple strategy for transdermal SH delivery.

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Section: Introductionmentioning

confidence: 99%

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

et al. 2020

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“…The physicochemical properties were determined, showing that Api m 1‐loaded microemulsion had excellent resistance to dermal proteases‐mediated degradation. Both its penetrating efficacy and in vivo availability were confirmed . Understating the microemulsion based on its principles, such as phase behavior, protein incorporation, and its formulation approach, characterization methods, etc., would be required for the transdermal delivery of protein therapeutics via a microemulsion system.…”

Section: Adjuvants For the Transdermal Delivery Of Protein Therapeuticsmentioning

confidence: 89%

Recent Advances in the Transdermal Delivery of Protein Therapeutics with a Combinatorial System of Chemical Adjuvants and Physical Penetration Enhancements

Park

Lee

et al. 2020

Advanced Therapeutics

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Since the development of protein‐based therapeutics, research has been underway to deliver protein therapeutics into the systemic circulation and target sites have been actively conducted. Most protein‐based therapeutics require parenteral administration, due to their intrinsic vulnerability and susceptibility to enzyme‐mediated degradation. Among the routes of administration, the transdermal delivery system has been regarded as a promising technique to deliver protein therapeutics, offering the advantages of painless administration, ease of termination, and avoidance of first‐pass metabolism. However, unlike small molecular drugs, protein therapeutics have limited skin penetration, due to their macromolecular and hydrophilic properties. Both cheimcal adjuvants (CAs)‐treatment methods and physical penetration enhancer methods (PPEs) have been utilized to increase skin permeability for protein therapeutics. The CAs, which include chemical penetration enhancers and nanocarriers, permit the protein therapeutics to transport easily into the skin, by modifying the stratum corneum (SC) or fabricating their stable formulation. The PPEs, including iontophoresis, electroporation, and ultrasound, can improve the skin permeability of the therapeutic agent through disrupting the SC. In this review, the techniques of both chemical and physical enhancement methods are introduced and an overview of the latest approaches to the transdermal delivery of protein therapeutics is provided.

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“…Additionally, similar challenges, concerning surfactant concentrations, exist while developing SEDDSs destined for topical/transdermal drug delivery, as skin is also sensitive towards high surfactant concentrations [73,74]. Skin irritation reactions associated with surfactant exposure is linked to the capacity of surfactants to solubilise lipid membranes [75].…”

Section: Surfactantsmentioning

confidence: 99%

“…Nonetheless, it has been found that a surfactant concentration of approximately 30-60% w/w of an oral SEDDS formulation renders enhanced spontaneous emulsification within the gastrointestinal environment [33]. Additionally, similar challenges, concerning surfactant concentrations, exist while developing SEDDSs destined for topical/transdermal drug delivery, as skin is also sensitive towards high surfactant concentrations [73,74]. Skin irritation reactions associated with surfactant exposure is linked to the capacity of surfactants to solubilise lipid membranes [75].…”

Section: Surfactantsmentioning

confidence: 99%

“…However, reversed micelles do not necessarily contribute As demonstrated in Figure 3, areas of a pseudo-ternary-phase diagram comprising either extensively high concentrations of the water-, oil-, or surfactant phase (combination of surfactant and co-surfactant) must be avoided, as these regions tend to generate unique structures such as lamellar phase formation in the presence of increased surfactant phase concentrations [100]. In addition, regions comprising increased surfactant concentrations must also be avoided to prevent skin irritation upon application of the drug delivery vehicle [73,74]. Moreover, reversed micelles are observed in oil rich regions of pseudo-ternary-phase diagrams [100].…”

Section: Pseudo-ternary Phase Diagrams Formerly Utilised Diagrams Wimentioning

confidence: 99%

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Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

2020

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Self-emulsifying drug delivery systems (SEDDSs) originated as an oral lipid-based drug delivery system with the sole purpose of improving delivery of highly lipophilic drugs. However, the revolutionary drug delivery possibilities presented by these uniquely simplified systems in terms of muco-adhesiveness and zeta-potential changing capacity lead the way forward to ground-breaking research. Contrarily, SEDDSs destined for topical/transdermal drug delivery have received limited attention. Therefore, this review is focused at utilising principles, established during development of oral SEDDSs, and tailoring them to fit evaluation strategies for an optimised topical/transdermal drug delivery vehicle. This includes a detailed discussion of how the authentic pseudo-ternary phase diagram is employed to predict phase behaviour to find the self-emulsification region most suitable for formulating topical/transdermal SEDDSs. Additionally, special attention is given to the manner of characterising oral SEDDSs compared to topical/transdermal SEDDSs, since absorption within the gastrointestinal tract and the multi-layered nature of the skin are two completely diverse drug delivery territories. Despite the advantages of the topical/transdermal drug administration route, certain challenges such as the relatively undiscovered field of skin metabolomics as well as the obstacles of choosing excipients wisely to establish skin penetration enhancement might prevail. Therefore, development of topical/transdermal SEDDSs might be more complicated than expected.

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Development of a skin-friendly microemulsion for dermal allergen-specific immunotherapy

Cited by 16 publications

References 37 publications

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

Polyvinylpyrrolidone microneedles for localized delivery of sinomenine hydrochloride: preparation, release behavior of in vitro & in vivo, and penetration mechanism

Recent Advances in the Transdermal Delivery of Protein Therapeutics with a Combinatorial System of Chemical Adjuvants and Physical Penetration Enhancements

Development of Topical/Transdermal Self-Emulsifying Drug Delivery Systems, Not as Simple as Expected

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