Cyclodextrin based nanosponge of norfloxacin: Intestinal permeation enhancement and improved antibacterial activity

Abstract

Nanosponges are a novel class of hyperbranched cyclodextrin-based nanostructures that exhibits remarkable potential as a drug host system for the improvement in biopharmaceutical properties. This work aims the development of cyclodextrin-based nanosponge of norfloxacin to improve its physicochemical characteristics. β-cyclodextrin was used as base and diphenyl carbonate as crosslinker agent at different proportions to produce nanosponges that were evaluated by in vitro and in vivo techniques. The proportion cyclodextrin:crosslinker 1:2 M/M was chosen due to its higher encapsulation efficiency (80%), revealing an average diameter size of 40 nm with zeta potential of -19 mV. Norfloxacin-loaded nanosponges exhibited higher passage of norfloxacin in comparison to norfloxacin drug alone by Ussing chamber method. The nanosponge formulation also revealed a mucoadhesive property that could increase norfloxacin absorption thus improving its antibiotic activity in an in vivo sepsis model. Therefore, nanosponges may be suitable carrier of norfloxacin to maximize and facilitate oral absorption.

<p>Improving the solubility and in vitro cytotoxicity (anticancer activity) of ferulic acid by loading it into cyclodextrin nanosponges</p>

“…FA-NSs did not show the endothermic point of FA that again confirms FA has been completely included into the NSs and also there is a tight interaction between CD and FA (Figure 5C). 26,8

Figure 5DSC thermograms of β-cyclodextrin nanosponges ( A ), ferulic acid ( B ), and ferulic acid-loaded nanosponges ( C ).

…”

“…Cyclodextrin-based nanosponges (CD-NSs) are nanoporous structures which are obtained through hyper cross-linking of the CDs using different cross-linkers. Recently, CD-NSs are specially used as innovative nanodelivery vehicles to enhance the water solubility of poorly soluble compounds,24,25 to improve their bioavailability,26 and to prolong the release of encapsulated compounds 27. CD-NSs can form colloidal nanosuspensions in aqueous solutions and enhance the release of bioactive compound 28.…”

Nanomedicine Fight against Antibacterial Resistance: An Overview of the Recent Pharmaceutical Innovations

“…Various kinds of self-assembled nonlamellar liquid crystalline nanoparticles have been recently evaluated for their potential as drug delivery systems for antimicrobial molecules [176]. The system consists of amphiphiles that orient themselves into different mesophase structures, for example hexagonal, lamellar, cubic, and the less common sponge structure [177,178]. Advantages of these nanosystems include their amphiphilic nature and their larger interfacial surface areas, which enable them to encapsulate both hydrophilic and hydrophobic drugs, in addition to the ease of production with the ability to scale-up.…”

Cyclodextrin‐Based Nanosponges for Improving Solubility and Sustainable Release of Curcumin

“…Biodegradability, biocompatibility, stability in the pH of 1–11 and negligible toxicity of NSs rendered them as safe drug carriers . To date, NSs have been used for delivery of various drugs such as Rilpivirine, Rosuvastatin calcium, Acyclovir, Norfloxacin, Anti‐restenotic Agent DB103, Doxorubicin and Captopril, Efavirenz, Nifedipine, Camptothecin, Paclitaxel and Curcumin …”