Cellulose Nanofibers Improve the Performance of Retrograded Starch/Pectin Microparticles for Colon-Specific Delivery of 5-ASA.

Andréia Bagliotti Meneguin,Maurício Palmeira Chaves De Souza,Marlus Chorilli,Rafael Miguel Sábio,Anselmo Gomes De Oliveira,Richard Perosa Fernandes

doi:10.3390/pharmaceutics13091515

Andréia Bagliotti Meneguin, Maurício Palmeira Chaves De Souza + Show 4 more

Open Access

https://doi.org/10.3390/pharmaceutics13091515

Copy DOI

Journal: Pharmaceutics	Publication Date: Sep 19, 2021
Citations: 12	License type: CC BY 4.0

Affiliation: Universidade Estadual Paulista (Unesp)

Abstract

Cellulose nanofibers (CNF) were employed as the nanoreinforcement of a retrograded starch/pectin (RS/P) excipient to optimize its colon-specific properties. Although starch retrogradation ranged from 32 to 73%, CNF addition discretely disfavored the RS yield. This result agrees with the finding that in situ CNF reduces the presence of the RS crystallinity pattern. A thermal analysis revealed that the contribution of pectin improves the thermal stability of the RS/CNF mixture. Through a complete factorial design, it was possible to optimize the spray-drying conditions to obtain powders with high yield (57%) and low moisture content (1.2%). The powders observed by Field Emission Gum Scanning Electron Microscopy (FEG-SEM) had 1–10 µm and a circular shape. The developed methodology allowed us to obtain 5-aminosalicilic acid-loaded microparticles with high encapsulation efficiency (16–98%) and drug loading (1.97–26.63%). The presence of CNF in RS/P samples was responsible for decreasing the burst effect of release in simulated gastric and duodenal media, allowing the greatest mass of drug to be targeted to the colon. Considering that spray-drying is a scalable process, widely used by the pharmaceutical industry, the results obtained indicate the potential of these microparticles as raw material for obtaining other dosage forms to deliver 5-ASA to the distal parts of gastrointestinal tract, affected by inflammatory bowel disease.

Highlights

Cellulose nanofibers (CNF) were employed as the nanoreinforcement of a retrograded starch/pectin (RS/P) excipient to optimize its colon-specific properties
It has been considered the drug of choice in the treatment of mild to moderate inflammatory bowel disease (IBD) [1], a set of autoimmune diseases characterized by chronic intestinal inflammations with causes not fully clarified [2] and whose main entities are ulcerative colitis and Crohn’s disease
In order to optimize the performance of an RS/P-based colonic excipient, CNF was added as a nanofiller for further building nanocomposite microparticles via spray drying

Summary

Introduction

Cellulose nanofibers (CNF) were employed as the nanoreinforcement of a retrograded starch/pectin (RS/P) excipient to optimize its colon-specific properties. Starch retrogradation ranged from 32 to 73%, CNF addition discretely disfavored the RS yield. This result agrees with the finding that in situ CNF reduces the presence of the RS crystallinity pattern. 5-Aminosalicylic acid (5-ASA) is a non-steroidal anti-inflammatory drug belonging to the aminosalicylates class. Considering the fast and extensive absorption of 5-ASA in the upper regions of the gastrointestinal tract (GIT) after oral administration, only an extremely low concentration of drug reaches the colon, reducing the local therapeutic effect [3]. The incidence of side effects after the rapid absorption of the drug in the upper portions of the GIT, such as diarrhea, nausea, abdominal pain, headache, vomiting and rash, frequently limit the patient’s adherence to treatment

Methods

Results

Conclusion