Chitosan in Oral Drug Delivery Formulations: A Review

Abstract

Nanoformulations have become increasingly useful as drug delivery technologies in recent decades. As therapeutics, oral administration is the most common delivery method, although it is not always the most effective route because of challenges with swallowing, gastrointestinal discomfort, low solubility, and poor absorption. One of the most significant barriers that medications must overcome to exert a therapeutic effect is the impact of the first hepatic transit. Studies have shown that controlled-release systems using nanoparticles composed of biodegradable natural polymers significantly improve oral administration, which is why these materials have attracted significant attention. Chitosan possesses a wide variety of properties and functions in the pharmaceutical as well as healthcare industries. Drug encapsulation and transport within the body are two of its most important features. Moreover, chitosan can enhance drug efficacy by facilitating drug interaction with target cells. Based on its physicochemical properties, chitosan can potentially be synthesized into nanoparticles, and this review summarizes recent advances and applications of orally delivered chitosan nanoparticle interventions.

Introduction

In recent decades, there has been increased interest in developing innovative methods to deliver drugs. In this review, we will discuss the pros and cons of drug delivery systems, the basic as well as physicochemical characteristics that could render a drug suitable for pharmaceutical formulation, and the techniques used to assess delivery sustainability, toxicity at the site of delivery, and its feasibility [1]. Despite the abundance of research on various methods for administering drugs, oral administration is still the most efficient, least complicated, and safest [2,3]. The advent of nanotechnology, and particularly, the field of nanomedicine, has increased the acceptance of nanocarriers as oral drug delivery vehicles, thereby overcoming these restrictions. The utilization of nanometric particles is at the core of nanomedicine, which is considered a branch of nanotechnology [4]. Numerous types of drug delivery systems make use of nanoparticles (NPs) as drug carriers. The pharmaceutical industry has found NPs to be useful for treating diseases such as cancer, diabetes, and HIV [5,6]. In order to improve therapeutic constraints and membrane crossing, NPs were developed. There is concern that some of the synthetic compounds used in these products present health risks to individuals [7]. Nanoparticles developed from polymers, such as chitosan NPs, and the infusion of herbal bioactives (Curcumin, aloe vera, etc.) possess desirable properties and applications because of their inherent versatility, biological compatibility, and biodegradability (Figure 1) [8,9].

There are a wide variety of polymers, both natural, synthetic, and semisynthetic, that can be used to formulate nanoparticles for various drug delivery [10]. Chitosan and its derivatives are distinguished from other polymers because of their superior characteristics, making them ideal for oral administration [11]. The addition of amino groups imparts a cationic charge, which enhances penetration and acts as a mucoadhesive [12]. These NPs are also non-toxic, biocompatible, and biodegradable. The biopolymer chitosan (CS) has gained significant attention in the medical field because of its versatility, availability, and unique properties. The linear polysaccharide chitosan is comprised of N-acetyl-D-glucosamine and D-glucosamine units that are randomly repeated and linked together via (1→4) glycosidic linkages [13]. Chitin is the source of chitosan, a natural polymer that is second only to cellulose in natural abundance. Chitin and chitosan are widely used in various industries, including the food industry as well as medical and pharmaceutical fields (i.e., tissue engineering, gene transplantation, and wound healing) [14]. Chitosan nanoparticles (CSNPs) have intriguing properties, particularly for ocular and oral distribution. Some active components are not very stable or bioavailable; however, CSNPs are considered a promising vehicle for improving these factors. To enhance retention and cellular uptake, chitosan can adhere strongly to the negatively charged mucus membrane [15]. Interestingly, many research studies were published related to chitosan drug delivery in the last few years. Recently, Guadarrama-Wacobar et al. 2023, reported chitosan-based oral delivery, mostly covering 2020 research data, and we focused on most of the research data that includes references from 2022 onwards. Now, we have reorganized our manuscript with the following subheadings, namely Introduction, Oral drug delivery, Nanotechnology in delivery systems, Applicability of chitosan-oriented multifarious delivery, Role of P-gp inhibitors in oral drug delivery, herbal bioactive-loaded nanoformulations in oral drug delivery, Patents, Future perspectives, and Conclusion.

The manuscript is structured based on the recent advancements targeting different chitosan-based oral nanodrug delivery systems in a concise way that covers most of the relevant areas.

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Sangnim, T.; Dheer, D.; Jangra, N.; Huanbutta, K.; Puri, V.; Sharma, A. Chitosan in Oral Drug Delivery Formulations: A Review. Pharmaceutics 2023, 15, 2361. https://doi.org/10.3390/pharmaceutics15092361

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