Advances in orally targeted drug delivery to colon

Belali, Nagina; Wathoni, Nasrul; Muchtaridi, Muchtaridi

doi:10.4103/japtr.japtr_26_19

Cited by 40 publications

(5 citation statements)

References 48 publications

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“…The size of the polymer also affects this behaviour, as it affects the surface area available for fluid penetration. The ability to control this behaviour encourages the use of polymers in many pharmaceutical drug delivery systems [1][2][3][4][5][6][7]. The pellets' swelling was examined in phosphate-buffered saline (PBS).…”

Section: Pellets' Swelling Assessmentmentioning

confidence: 99%

“…Targeted drug delivery to the colon has attracted the attention of many researchers owing to its tremendous advantages over systemic drug administration, including increased drug potency and efficacy and reduced adverse drug reactions [1,2]. Colonic drug delivery systems have been used to treat a plethora of bowel diseases encompassing colorectal carcinoma, ulcerative colitis, diverticulitis, Crohn's disease, and irritable bowel syndrome [3][4][5].…”

Section: Introductionmentioning

confidence: 99%

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Smart Pellets for Controlled Delivery of 5-Fluorouracil

et al. 2022

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This work aimed to develop a new one-pot and readily scaled-up formulation capable of retaining 5-fluorouracil and prolonging its release to obtain a site-specific medication delivery for the potential treatment of colorectal cancer. Six polymer-based formulations were successfully produced using a thermal bulk polymerization method and loaded with 5-fluorouracil, which is a chemotherapeutic agent used in the treatment of colorectal carcinoma. The pellets produced were characterized by measuring the glass transition temperature, tensile strength, Young’s modulus, and tensile elongation at break. Studies on in vitro swelling and release were carried out in phosphate-buffered saline to evaluate the behaviour of the developed system. The Young’s modulus, glass transition temperature, and tensile strength all increased significantly as the crosslinker concentration increased, but the fracture strain value reduced significantly. The in vitro swelling profile of the produced formulations was significantly reduced by increasing crosslinking density. Less than 27% cumulative drug release was achieved for all formulations after 5 h of starting the release study. The highest cumulative drug release reached after 24 h was 69%. The developed drug delivery system demonstrated the ability to delay the release of 5-fluorouracil in upper gastrointestinal tract-mimicking conditions, while permitting its release in a controlled way afterward, which makes it promising for the potential delivery of 5-fluorouracil to the colon.

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Section: Pellets' Swelling Assessmentmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Smart Pellets for Controlled Delivery of 5-Fluorouracil

et al. 2022

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“…Some materials are resistant to gastric digestion (e.g., cellulose and cellulose derivates, resistant starch, some pectins and alginates, etc.) and serve for release of active compounds in the colon, being exposed to subsequent microbial degradation (Belali et al, 2019). Many reports stressed that gut microbial transformation could potentially improve the therapeutic effects of plant bioactive products, including EOs and particular terpenoids (Wang et al, 2019).…”

Section: Carriers Disintegration Under Gastric Conditionsmentioning

confidence: 99%

Natural Macromolecules as Carriers for Essential Oils: From Extraction to Biomedical Application

Stevanović

Sieniawska

Głowniak

et al. 2020

Front. Bioeng. Biotechnol.

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Essential oils (EOs) and their main constituents, the terpenes, are widely studied, mostly relating to their antioxidant ability and bioactivity, such as antimicrobial, anticancer, anti-inflammatory, and range of other actions in the living systems. However, there is limited information on their bioavailability, especially upon clinical studies. Having in mind both strong biological effects and health benefits of EOs and their specific physicochemical properties (volatility, lipophilic character, low water solubility or insolubility, viscosity, expressed odor, concentration-dependent toxicity, etc.), there is a need for their encapsulation for target delivery. Encapsulation of EOs and their constituents is the prerequisite for enhancing their oxidative stability, thermostability, photostability, shelf life, and biological activity. We considered various carrier types such a (1) monophase and polyphase polysaccharide hydrogel carriers, (2) polysaccharide-protein carriers, and (3) lipid carriers in the context of physicochemical and engineering factors. Physicochemical factors are encapsulation efficiency, chemical stability under gastric conditions, mechanical stability, and thermal stability of carrier matrices. Choice of carrier material also determines the encapsulation technique. Consequently, the engineering factors are related to the advantage and disadvantage of various encapsulation techniques frequently used in the literature. In addition, it was intended to address the interactions between (1) main carrier components, such as polysaccharides, proteins, and lipids themselves (in order to form chemically and mechanically stable structure); (2) main carrier components with pepsin under gastric conditions (in order to form resistant material under gastric conditions); and (3) main carrier components with EOs (in order to enhance encapsulation efficiency), as a necessary precondition for whole process optimization. Finally, different sources for obtaining natural carrier macromolecules are surveyed, especially the agro-waste materials and agricultural and food by-products. This review article highlights the bioavailability aspects of encapsulated EOs and physicochemical and engineering factors concerning natural macromolecule carriers for their target delivery and application.

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“…Mucoadhesion permits localized drug delivery, enabled by the high intestinal permeability of nanoparticles, which accumulate in specific intestinal sections. This strategy enhances drug bioavailability, reduces systemic toxicity, and increases patient compliance [21][22][23].…”

Section: Introductionmentioning

confidence: 99%

Co-encapsulation of curcumin and salicylic acid in mucoadhesive polymer nanoparticles

Moreno,

Forero,

Baena

et al. 2023

J Appl Pharm Sci

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Colorectal cancer poses a significant global health challenge with high incidence and mortality rates, as reported by the World Health Organization. Natural compounds such as curcumin (Cur) and salicylic acid (SCA) have shown promising therapeutic effects against colorectal cancer. However, their oral administration is hindered by their low bioavailability. This study aimed to develop mucoadhesive nanoparticles capable of co-encapsulating Cur and SCA using a double-emulsion process. The copolymer m-PEG-b-PCL, which is considered a safe material for biomedical applications, was chosen as the polymeric precursor, while chitosan, which has mucoadhesive properties, served as the emulsion stabilizer. Through the optimization of drug concentrations, polymer molecular weights, and stabilizer type and concentration, a formulation composed of spherical nanoparticles with an average hydrodynamic diameter of 355 nm and an entrapment efficiency of 13.70% for Cur and 90.72% for SCA was obtained. The release kinetics showed sustained release over 24 hours. Moreover, these nanoparticles demonstrated strong adhesion to the colonic mucosa, presenting a potential localized drug delivery strategy. Co-encapsulation of Cur and SCA within mucoadhesive polymer nanoparticles holds great potential for significantly enhancing the therapeutic outcomes of colorectal cancer treatment.

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Advances in orally targeted drug delivery to colon

Cited by 40 publications

References 48 publications

Smart Pellets for Controlled Delivery of 5-Fluorouracil

Smart Pellets for Controlled Delivery of 5-Fluorouracil

Natural Macromolecules as Carriers for Essential Oils: From Extraction to Biomedical Application

Co-encapsulation of curcumin and salicylic acid in mucoadhesive polymer nanoparticles

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