Abstract

(1) Background: In the treatment of ulcerative colitis (UC), accurate delivery and release of anti-inflammatory drugs to the site of inflammation can reduce systemic side effects. (2) Methods: We took advantage of this goal to prepare resveratrol-loaded PLGA nanoparticles (RES-PCAC-NPs) by emulsification solvent volatilization. After layer-by-layer self-assembly technology, we deposited chitosan and alginate to form a three-layer polyelectrolyte film. (3) Results: It can transport nanoparticles through the gastric environment to target inflammation sites and slowly release drugs at a specific pH. The resulting RES-PCAC-NPs have an ideal average diameter (~255 nm), a narrow particle size distribution and a positively charged surface charge (~13.5 mV). The Fourier transform infrared spectroscopy showed that resveratrol was successfully encapsulated into PCAC nanoparticles, and the encapsulation efficiency reached 87.26%. In addition, fluorescence imaging showed that RES-PCAC-NPs with positive charges on the surface can effectively target and accumulate in the inflammation site while continuing to penetrate downward to promote mucosal healing. Importantly, oral RES-PCAC-NPs treatment in DSS-induced mice was superior to other results in significantly improved inflammatory markers of UC. (4) Conclusions: Our results strongly prove that RES-PCAC-NPs can target the inflamed colon for maximum efficacy, and this oral pharmaceutical formulation can represent a promising formulation in the treatment of UC.

Highlights

  • One goal of medicine is to find new drugs to replace drugs with limited efficacy, but drug development is a time-consuming and expensive process

  • RES-loaded nanoparticles are prepared with the castor oil derivative “propenol oil” as a RES-loaded nanoparticles are prepared with the castor oil derivative “propenol oil” as a non-toxic solvent [57], β-lactoglobulin as the main molecule [58] and silk fibroin as the non-toxic solvent [57], β-lactoglobulin as the main molecule [58] and silk fibroin as the outer shell [59], and a liquid crystal structure based on glyceryl oleate encapsulates theraouter shell [59], and a liquid crystal structure based on glyceryl oleate encapsulates therpeutic proteins and small molecule antioxidants [60]

  • We verified that RES-PCAC-NPs are less released at a low pH and slowly released at a high pH, which can protect the drug from passing through the stomach to the colon

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Summary

Introduction

One goal of medicine is to find new drugs to replace drugs with limited efficacy, but drug development is a time-consuming and expensive process. The most effective sources of medicines are natural products, which can be identified through analytical techniques, such as high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS) [1]. The analytical methods commonly used for IBD treatment include the fabric phase sorptive extraction-high performance liquid chromatographyphotodiode array detection method (FPSE-HPLC-PDA), which can be used to determine residual IBD drugs [3]. It provides a guarantee for the effective treatment of IBD. IBD includes UC and Crohn’s disease [4,5]. UC is characterized by abdominal pain, diarrhea and bleeding, which will have a negative effect on all life activities of the patient [6]

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