Table 2.
Studies on the formula, preparation method and biological activity of different microparticles in treating UC.
| Categories | Carrier Materials | Loaded-Ingredients | Preparation Methods | Biological Activity | Ref. |
|---|---|---|---|---|---|
| Microsphere | Chitosan-alginate | Icariin | Emulsification-internal gelation technique | Exert the colon-protective effects through reducing the inflammatory response | [50] |
| Microsphere | Eudragit S100 liquid paraffin | Metronidazole | Emulsification solvent-evaporation method | Enhance drug entrapment, and effect the drug release | [51] |
| Microsphere | PLGA microsphere | Glucagon-like peptide-2 | Solid-in-oil-in-water (S/O/W) method | Resistant to degradation and decreased the severity of dextran sulfate sodium (DSS)-induced ulcerative colitis | [52] |
| Microspheric vehicle | Microspheric vehicle formed by cationic konjac glucomannan (cKGM), phytagel | An antisense oligonucleotide against TNF-α | Water-in-oil (W/O) emulsion method | Significantly decreased the local level of TNF-α and alleviated the symptoms of colitis in the mice | [53] |
| Microsphere | pH-triggered Eudragit-coated chitosan microspheres | Curcumin | Emulsion crosslinking method followed by coating with Eudragit S-100 | A promising system for pH-dependent delivery of drug to colon in ulcerative colitis | [54] |
| Microsphere | The enzyme diamine oxidase (DAO) in CaCMS/alginate microspheres | The enzyme diamine oxidase (DAO) | --- | A procedure able to afford protection of the entrapped enzyme against gastrointestinal degradation | [55] |
| Microsphere | Colon-targeted microspheres which were compressed into tablets using the enzyme-dependent polymer (pectin) as coat | The nonsteroidal anti-inflammatory bumadizone calcium dihydrate | Quasi-emulsion solvent-diffusion method | Achieved significant decrease in myeloperoxidase activity and inflammation with delayed Tmax (4 h) and lower Cmax (2700 ng/mL) when compared to marketed product | [56] |
| Microsphere | Hydrogel microspheres of chitosan grafted with vinyl polymers | 5-Aminosalicylic acid (5-ASA) | Water-in-oil (W/O) emulsification method | Exhibited better therapeutic effects in comparison to 5ASA plain drug solution in oral administration | [57] |
| Microsphere | Chitosan microspheres | 5-ASA and camylofine dihydrochloride | Emulsion method followed by enteric coating with Eudragit® S-100 | Specific delivery of drug to the colon and reduce symptoms of ulcerative colitis | [58] |
| Microsphere | Eudragit L100 (EuL)-coated chitosan (Ch)–succinyl-prednisolone (SP) conjugate microspheres (Ch SP-MS/EuL) | Prednisolone (PD) | --- | Enhanced effectiveness of PD and reduced toxic side effects of PD greatly | [59] |
| Microsphere | Budesonide (BUD) guar gum microspheres | Budesonide (BUD) | Emulsion crosslinking technique | Prolong the acting time of BUD in vivo | [60] |
| Microsphere | Chitosan microparticles | Mesalamine | Emulsion chemical crosslinking technique | Maintain the drug concentration within target ranges for a long period of time | [61] |
| Microparticle | Kafrin microparticles | Prednisolone | A phase-separation method | The majority of the loaded prednisolone was not released in in-vitro conditions simulating the upper gastrointestinal tract | [62] |
| Microparticle | N-Succinyl-chitosan (SucCH) microparticle | 5-ASA | Spray-drying method | Improved efficacy in the healing of induced colitis in rats | [63] |
| Microsphere | pH-sensitive microspheres using Eudragit P4135F | Low-molecular-weight heparins (LMWH) | A double emulsion technique with either solvent extraction or evaporation | Exhibited a particle size adapted to the needs of inflammatory bowel disease therapy, an efficient LMWH encapsulation, and a pH-controlled drug release | [64] |
| Microparticle | Poly-ε-caprolactone (PCL) celecoxib-loaded microparticles | Celecoxib | Solvent-diffusion technique | Enhanced the bioavailability and extended the duration of drug-plasma concentration in rats | [65] |