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Tributyrin (TB), a stable triglyceride prodrug of butyrate, holds immense potential for modulating gut health and managing ulcerative colitis (UC) via dietary intervention. However, its application in functional foods is restricted by its hydrophobicity, gastric instability, and rapid absorption in the upper gastrointestinal tract (GIT). To address these challenges, this study engineered a food‐grade, colon‐specific delivery system based on hierarchical emulsion‐filled hydrogel microbeads. TB was initially stabilized by octenyl succinic anhydride (OSA)‐modified Tartary buckwheat starch to form robust Pickering emulsions (OSP), which were subsequently embedded within a pH‐responsive sodium alginate (SA)/carboxymethyl chitosan (CMCS) composite matrix. The intermolecular polyelectrolyte complexation between SA and CMCS, reinforced by Ca2+‐mediated crosslinking, significantly enhanced the structural integrity and encapsulation efficiency (∼64%) of the microbeads (TB‐OSP@C/S). In vitro digestion kinetics demonstrated that this multi‐compartment architecture acted as an effective diffusion barrier, suppressing gastric release (< 20%) while facilitating sustained release in the simulated colonic environment driven by pH‐dependent swelling and the enzymatic degradation of the protective starch shell. In a DSS‐induced murine colitis model, oral administration of TB‐OSP@C/S microbeads markedly improved the disease activity index, alleviated colonic tissue damage, and exhibited superior anti‐inflammatory efficacy compared to free TB. This work presents a facile, surfactant‐free strategy for the precise delivery of hydrophobic nutraceuticals, offering a promising paradigm for developing precision nutrition products targeting intestinal inflammation. Hierarchical emulsion‐filled hydrogel microbeads were constructed via polyelectrolyte complexation for the colon‐targeted delivery of tributyrin. This system effectively minimizes gastric loss while enabling precise colonic release to alleviate colitis, providing a robust platform for functional dietary interventions.

The aim of this study was to design, optimize, and develop metronidazole (Met) loaded nanoparticles (MetNp) by employing quality-based design (QbD) as well as a risk assessment methodology. A fractional factorial design was used by selecting five independent variables viz., chitosan concentration, tripolyphosphate concentration, and acetic acid concentration as material attributes, stirring speed, and stirring time as process parameters, whereby their influence on two dependent variables such as particle size (PS) and %entrapment efficiency (%EE) was studied. MetNp were synthesized by employing an ionic-gelation technique and optimized formula obtained from the QbD design study. PS and %EE studies revealed the formation of MetNp with 558.06 ± 2.52 nm and 59.07 ± 2.15%, respectively. Furthermore, a Met release study in various simulated gastro-intestinal media suggested pH-triggered (pH > 7.0) and sustained release profile of Met from Eudragit S100 enteric-coated MetNp capsule (MetNp cap). Moreover, the stability investigation of formulations confirmed good stability with respect to their PS and residual drug content (RDC) at different temperature conditions. In conclusion, the QbD method was effectively utilized in the development of MetNp and enteric-coated MetNp cap depicting their potential to release Met through MetNp cap only in the colon region and can be utilized for the treatment of amoebiasis in the colon.

Pulsatile drug delivery systems (PDDS) are getting prime importance in the field of pharmaceutical sciences as these systems deliver the right dose at specific time at a specific site. In pulsatile drug delivery system the drug is released rapidly after a well defined lag-time. It could be advantageous for many drugs or conditions. A pulse has to be designed in such a way that a complete and rapid drug release is achieved after the lag time so as to match body's circadian rhythms with the release of drug which increases the efficacy and safety of drugs by proportioning their peak plasma concentrations during the 24 hours in synchrony with biological rhythm. Pulsatile release systems can be classified in multiple-pulse and single-pulse systems. This article mainly focus on different approaches for colon specificity, various techniques available for the pulsatile delivery like pH dependent systems, time dependent systems, etc. A popular class of single-pulse systems is that of rupturable dosage forms. Advantages of the pulsatile drug delivery system are reduced dose frequency; reduce side effects, drug targeting to specific site like colon and many more. Now in market varies technologies of pulsatile drug delivery system like Pulsincap, Diffucaps etc. are launched by pharmaceutical companies.

An enzyme-responsive colon-specific delivery system was developed based on hollow mesoporous silica spheres (HMSS) to which biodegradable chitosan (CS) was attached via cleavable azo bonds (HMSS–N=N–CS). Doxorubicin (DOX) was encapsulated in a noncrystalline state in the hollow cavity and mesopores of HMSS with the high loading amount of 35.2%. In vitro drug release proved that HMSS–N=N–CS/DOX performed enzyme-responsive drug release. The grafted CS could increase the biocompatibility and stability and reduce the protein adsorption on HMSS. Gastrointestinal mucosa irritation and cell cytotoxicity results indicated the good biocompatibility of HMSS and HMSS–N=N–CS. Cellular uptake results indicated that the uptake of DOX was obviously increased after HMSS–N=N–CS/DOX was preincubated with a colonic enzyme mixture. HMSS–N=N–CS/DOX incubated with colon enzymes showed increased cytotoxicity, and its IC50 value was three times lower than that of HMSS–N=N–CS/DOX group without colon enzymes. The present work lays the foundation for subsequent research on mesoporous carriers for oral colon-specific drug delivery.

Curcumin’s role in the treatment of ulcerative colitis (UC) has been proven by numerous studies, but its preventive administration, with the aim of reducing the remission episodes that are characteristic of this disease, must be further investigated. This study investigates the effects of a novel curcumin-loaded polymeric microparticulate oral-drug-delivery system for colon targeting (Col-CUR-MPs) in an experimental model of UC. Male Wistar rats (n = 40) were divided into five groups (n = 8), which were treated daily by oral gavage for seven days with a 2% aqueous solution of carboxymethylcellulose sodium salt (CMCNa) (healthy and disease control), free curcumin powder (reference), Col-CUR-MPs (test) and prednisolone (reference) prior to UC induction by the intrarectal administration of acetic acid (AA), followed by animal sacrification and blood and colonic samples’ collection on the eighth day. Col-CUR-MPs exhibited an important preventive effect in the severity degree of oxidative stress that resulted following AA intrarectal administration, which was proved by the highest catalase (CAT) and total antioxidant capacity (TAC) levels and the lowest nitrites/nitrates (NOx), total oxidative status (TOS) and oxidative stress index (OSI) levels. Biochemical parameter analysis was supported by histopathological assessment, confirming the significant anti-inflammatory and antioxidant effects of this novel colon-specific delivery system in AA-induced rat models of UC. Thus, this study offers encouraging perspectives regarding the preventive administration of curcumin in the form of a drug delivery system for colon targeting.

Compelling data have indicated menopause-associated increase in cardiovascular disease in women, while the underlying mechanisms remain largely unknown. It is established that changes of intestinal microbiota affect cardiovascular function in the context of metabolic syndrome. We here aimed to explore the possible link between host intestinal function, microbiota, and cardiac function in the ovariectomy (OVX) mouse model. Mice were ovariectomized to induce estrogen-related metabolic syndrome and cardiovascular defect. Microbiota was analyzed by 16s rRNA sequencing. miRNA and mRNA candidates expression were tested by qPCR. Cardiac function was examined by echocardiography. Colon specific delivery of miRNA candidates was achieved by oral gavage of Eudragit S100 functionalized microspheres. In comparison with the sham-operated group, OVX mice showed compromised cardiac function, together with activated inflammation in the visceral adipose tissue and heart. Lactobacillus abundance was significantly decreased in the gut of OVX mice. Meanwhile, miR-155 was mostly upregulated in the intestinal epithelium and thus the feces over other candidates, which in turn decreased Lactobacillus abundance in the intestine when endocytosed. Oral delivery of miR-155 antagonist restored the protective microbiota and thus protected the cardiac function in the OVX mice. This study has established a possible regulatory axis of intestinal miRNAs-microbiota-estrogen deficiency related phenotype in the OVX model. Colon specific delivery of therapeutic miRNAs would possibly restore the microbiota toward protective phenotype in the context of metabolic syndrome.

Ulcerative colitis (UC) is a non-specific inflammatory intestinal disease with long course and easy recurrence, which is one of the refractory diseases. In the previous work, -quinone methide compound -QM- was found to be a potential anti-UC drug in UC mice; however, its water solubility was poor, and the oral dosage was high. In this study, in response to these shortcomings, an oral, actively targeted, and drug-loaded nanostructured lipid carrier (NLC) was constructed, and the dual-stage targeted design was performed on it. Firstly, the -QM- -loaded NLC surface was modified with infliximab (IFX) ( -QM- -IFX-NLC), which can target highly expressed TNF-α in inflammatory cells or tissues; secondly, -QM- -IFX-NLC was coated with Eudragit S100 (S100- -IFX-NLC), which can achieve specific release in the colon and protect NLC from interference from the gastrointestinal environment. The experimental results suggested that the dual-stage targeted design of S100- -IFX-NLC can effectively increase the solubility of -QM- , allowing S100- -IFX-NLC to target the colon and -QM- -IFX-NLC to target the inflammatory tissue, increasing the aggregation of -QM- in the colon, enhancing the efficacy of -QM- , reducing the usage of -QM- , and increasing safety. The construction of Eudragit S100-coated -QM- -loaded IFX-modified NLC (S100- IFX-NLC) was effective and can improve the therapeutic effect of free drugs on UC.

The rationale for the current investigation is to study the crude banana peel (CBP) powder efficiency as a novel natural time-dependent polymer along with a pH-sensitive polymer to develop flurbiprofen colon-specific tablets. The direct compression method is utilized to prepare the flurbiprofen-CBP matrix tablets using 9 mm punches on the rotary tableting machine and subsequently coated with Eudragit® S 100 by a dip coating method. The tablets were evaluated for various tableting properties and in vitro drug release studies. From the results of dissolution studies, the F6 formulation showed negligible drug release (5.76% in 5 h) in the upper gastrointestinal tract and progressive release in the colon (99.08% in 24 h). Mean dissolution time, T10%, and T80% were found to be 13.33 h, 5.8 h, and 20.7 h, respectively, which explains the efficiency of the present combination of polymers for colon-specific drug release. From the dissolution studies results of stability studies, the similarity index was calculated and found to be 74.75. In conclusion, utilizing CBP as a natural, time-dependent polymer in conjunction with Eudragit® S 100 to develop the flurbiprofen tablets seems like a promising approach for delivering drugs specifically to the colon. Graphical Abstract

Site-specific delivery of anticancer drugs into tumor cells increase therapeutic efficacy while decreasing unwanted side effects. Oxaliplatin (Oxa) is a third-generation platinum derivative used to treat advanced colorectal cancer (CRC). Oxaliplatin-loaded bovine serum albumin nanoparticles (Nps-Bsa-Oxa) were formulated by a desolvation method. The Nps-Bsa-Oxa were characterized for their size, zeta potential (ZP), surface morphology and charge, in vitro Oxa release, release kinetics, in vitro cytotoxicity, and in vivo studies. The drug loading ranged from 8.39 ± 2.4%w/w to 13.86 ± 2.6w/w. The size and surface charge of the Nps-Bsa-Oxa was found to be 163.2 ± 6.3 nm and − 27 mV, respectively. The Oxa release was studied by dialysis, revealing a biphasic release pattern, and it varied from 48.84 ± 2.97 to 62.12 ± 2.74 for 24 h. In vitro cytotoxicity study was carried out by MTT assay using HT29 cell lines, and the Nps-Bsa-Oxa showed higher cytotoxicity when compared with free drug Oxa. The concentration of Oxa needed to inhibit the growth of 50% cells (IC 50 ) was comparatively less in the case of Nps (17.5 µg/ml) than free Oxa (24 µg/ml). In vivo studies on Wistar rats revealed that Nps-Bsa-Oxa delivered more Oxa to the colonic region compared to the free form of the drug Oxa.

PurposeThis study aims to overcome the challenges of the current oral targeted drug delivery system, such as the complex preparation process, poor biocompatibility, and delayed drug release.MethodsHere, a non-covalent polymer hydrogel was prepared using the mechanochemical method, and the solid phase loading of 5-amino salicylic acid (5-ASA) was realized.ResultsThe results obtained from the thermodynamics study, particle size analysis, and electron microscopy show that chitosan (CS) and sodium alginate (SA) form a pH-sensitive hydrogel under the mechanochemical force and also maintain good stability in aqueous solution. Fluorescent tracers study showed that the pH-sensitive hydrogel could achieve the targeted drug release in the colon and the retention time was over 12 h. Next, in vivo efficacy studies, change in mice body weight, DAI (disease activity index) score, thymus, and spleen index, and the diseased state of the mice colon revealed that the pH-sensitive hydrogel is an improved drug delivery system over 5-ASA API commercial preparations as observed in the efficacy and toxicological studies.ConclusionThis method uses an innovative preparation technology that without the need of cross-linking agent to produce an efficient colon-targeted drug delivery system for the treatment of ulcerative colitis.