Characterization of hyperbranched core‐multishell nanocarriers as an innovative drug delivery system for the application at the oral mucosa

Abstract

Background and Objectives In the oral cavity, the mucosal tissues may develop a number of different pathological conditions, such as inflammatory diseases (gingivitis, periodontitis) and autoimmune disorders (eg, oral lichen planus) that require therapy. The application of topical drugs is one common therapeutic approach. However, their efficacy is limited. Dilution effects due to saliva hinder the adherence and the penetration of drug formulations. Therefore, the bioavailability of oral topical drugs is insufficient, and patients may suffer from disease over years, if not life‐long. Material and Methods In the present study, we characterized core‐multishell (CMS) nanocarriers for their potential use as drug delivery systems at oral mucosal tissues. For this purpose, we prepared porcine masticatory as well as buccal mucosa and performed Franz cell diffusion experiments. Penetration of fluorescently labeled CMS nanocarriers into the mucosal tissue was analyzed using confocal laser scanning microscopy. Upon exposure to CMS nanocarriers, the metabolic and proliferative activity of gingival epithelial cells was determined by MTT and sulforhodamine B assays, respectively. Results Here, we could show that the carriers penetrate into both mucosal tissues, while particles penetrate deeper into the masticatory mucosa. Electron paramagnetic resonance spectroscopy revealed that the 3‐carboxy‐2,2,5,5‐tetramethyl‐1‐pyrrolidinyloxy‐labeled glucocorticoid dexamethasone loaded on to the CMS nanocarriers was released from the carriers in both mucosal tissues but with a higher efficiency in the buccal mucosa. The release from the nanocarriers is in both cases superior compared to the release from a conventional cream, which is normally used for the treatment of inflammatory conditions in the oral cavity. The CMS nanocarriers exhibited neither cytotoxic nor proliferative effects in vitro. Conclusion These findings suggested that CMS nanocarriers might be an innovative approach for topical drug delivery in the treatment of oral inflammatory diseases.

Electrospinning Nanofibers for Therapeutics Delivery

“…Of all delivery routes, the oral route is considered the most preferable and convenient route of administration, which can overcome the problems associated with other routes of administration [44]. However, to achieve successful administration of therapeutics targeting the oral route of administration is a difficult task.…”

Nanocrystals for Improved Drug Delivery of Dexamethasone in Skin Investigated by EPR Spectroscopy

“…First, the loading capacity with DxPCA and its localization in carrier system was characterized, followed by skin penetration investigations on ex vivo skin. During these investigations, Dx and DxPCA were found to be poorly soluble in aqueous solution [18][19][20].…”

NETs Are Double-Edged Swords with the Potential to Aggravate or Resolve Periodontal Inflammation

“…Clinically, the topical application of prednisolone alone [130] into the periodontal pocket in cases of periodontitis exacerbation is sufficient for a temporary resolution of periodontitis inflammation, or at least for its attenuation. Similarly, topical application of resolvin E1 in an animal model caused resolution of inflammation via PMN depriming [130]. These findings clearly indicate that the bacterial challenge in periodontitis plays a secondary role.…”

“…[138]. (iii) Topically applied prednisolone: corticosteroids downregulate NETs [139] and are efficient and prevalent medication in periodontology [130]. (iv) Doxycycline and its derivates are metalloproteinase inhibitors and efficiently downregulate the NET metalloproteinases in a sub-antimicrobial dose applied as a systemic adjunctive or a topical therapy [43].…”