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. 2021 Apr 22;13(5):608.
doi: 10.3390/pharmaceutics13050608.

Physico-Chemical and In Vitro Characterization of Chitosan-Based Microspheres Intended for Nasal Administration

Csilla Bartos  1 , Patrícia Varga  1 , Piroska Szabó-Révész  1 , Rita Ambrus  1
Affiliations

Physico-Chemical and In Vitro Characterization of Chitosan-Based Microspheres Intended for Nasal Administration

Csilla Bartos et al. Pharmaceutics. .

Abstract

The absorption of non-steroidal anti-inflammatory drugs (NSAIDs) through the nasal epithelium offers an innovative opportunity in the field of pain therapy. Thanks to the bonding of chitosan to the nasal mucosa and its permeability-enhancing effect, it is an excellent choice to formulate microspheres for the increase of drug bioavailability. The aim of our work includes the preparation of spray-dried cross-linked and non-cross-linked chitosan-based drug delivery systems for intranasal application, the optimization of spray-drying process parameters (inlet air temperature, pump rate), and the composition of samples. Cross-linked products were prepared by using different amounts of sodium tripolyphosphate. On top of these, the micrometric properties, the structural characteristics, the in vitro drug release, and the in vitro permeability of the products were studied. Spray-drying resulted in micronized chitosan particles (2-4 μm) regardless of the process parameters. The meloxicam (MEL)-containing microspheres showed nearly spherical habit, while MEL was present in a molecularly dispersed state. The highest dissolved (>90%) and permeated (~45 µg/cm2) MEL amount was detected from the non-cross-linked sample. Our results indicate that spray-dried MEL-containing chitosan microparticles may be recommended for the development of a novel drug delivery system to decrease acute pain or enhance analgesia by intranasal application.

Keywords: chitosan; meloxicam; microsphere; nasal administration; spray-drying.

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Conflict of interest statement

The authors declare no conflict of interest. The founding sponsors had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results.

Figures

Figure 1
Figure 1
Illustration of in vitro permeability investigation.
Figure 2
Figure 2
SEM images of spray-dried samples.
Figure 3
Figure 3
(a) DSC curves of PMs (Chit_MEL_2mlTPP-sol., Chit_MEL_1mlTPP-sol., Chit_MEL) and MEL-containing spray-dried samples; (b) XRPD patterns of PMs and MEL-containing spray-dried samples.
Figure 4
Figure 4
(a) FT-IR curves of the raw materials and the spray-dried samples without MEL, (b) FT-IR curves of the PMs and the MEL-containing spray-dried samples.
Figure 5
Figure 5
In vitro permeability of raw MEL and of MEL-containing spray-dried products.
See this image and copyright information in PMC

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