Electrosprayed microparticles for intestinal delivery of prednisolone

Abstract

Single and coaxial electrospraying was used to prepare Eudragit L100-55 polymer microparticles containing prednisolone as the active pharmaceutical ingredient. Different compositions of prednisolone and Eudragit L100-55 were used to develop five different formulations with different polymer : drug ratios. The resultant microparticles had a toroidal shape with a narrow size distribution. Prednisolone was present in an amorphous physical state, as confirmed by X-ray diffraction analysis. Dissolution studies were carried out in order to investigate the feasibility of the proposed system for site-specific release of prednisolone. The release rates were interpreted in terms of diffusion-controlled release. It was shown that utilization of pH-responsive Eudragit L100-55 could minimize the release of prednisolone in the acidic conditions of the stomach, which was followed by rapid release as the pH of the release medium was adjusted to 6.8 after the first 2 h. This is especially desirable for the treatment of conditions including inflammatory bowel disease and colon cancer.

Fabrication of Polymeric Microparticles by Electrospray: The Impact of Experimental Parameters

“…To date, there are a number of object types that have been employed and presented in the literature to serve as contacts between the liquid that is expelled from the syringe with the applied load from the voltage source. Some reports present a variety of denominations for the metal tip which is attached at the source, including a needle [12,13], nozzle [29,30], and capillary [31]. For a better understanding of these materials a schematic representative is depicted in Figure 2 according to some reports optimizing the ES settings.…”

“…The coaxial needle has an inner and an outer needle, as demonstrated in Figure 3b, and the technology is called CES [47,48]. This approach is commonly used to design polymeric MPs which can encapsulate a filler, for example, proteins [42,49], living yeast cells [50], and drugs [12,13,29,40]. In CES, two immiscible liquids or a liquid and a gas are injected into the outer and inner needles, with FRs controlled by two syringe pumps, respectively.…”

“…ES is a facile, simple and direct approach, and therefore, a promising technology for the engineering of MPs suitable for many translational applications. In addition, it is of significant importance for the biomedical field since it allows for the facile encapsulation of drugs in MPs [12,13], and the controlled processing of biodegradable polymeric MP [14]. In this review, we aim to discuss and highlight various parameters employed in ES technology for the manufacturing of polymeric MPs; their impact on MP properties; the influence of processing parameters such as polymer solvent, applied voltage, flow rate (FR), types of collectors, distance between the collector and the tip of the needles, etc.…”

AlCl<sub>3</sub> Cross-Linked and Spray Dried Carboxymethyl Sago Cellulose Microspheres as Potential Carriers for the Enteric Delivery

“…The IR spectrums of prednisolone and CMSC/Prednisolone physical mixture were presented in Figure 2. Both have shown characteristic bands of the OH group at 3200 -3500 cm −1 (OH involved in intermolecular association) confirms the presence of three hydroxyl groups of prednisolone [14]. The characteristic stretching vibrations of carbonyl groups C=O at 1700 cm −1 and C=C at 1660 cm −1 appear as very strong bands in the spectrum of prednisolone (Figure 2 Changes in the FT-IR spectrum due to interaction between CMSC and AlCl 3 were reported in our previous publication [2].…”

Formulation and Characterisation of a Combination Captopril and Hydrochlorothiazide Microparticulate Dosage Form

“…It is likely that the low turbulence observed at low agitation speeds may have resulted in loss of HCTZ from the dispersed phase resulting in a lower EE, as previously reported [29]. Increasing the Eud ® E100 content resulted in a slight decrease in the % HCTZ released at 30 min due to an increase in the thickness of the microparticle wall and consequently the diffusional path length of HCTZ as discussed in Section 3.2.4 [30][31][32]. Moreover, the solubility of Eud ® E100 in gastric fluids of pH <5 can be used to facilitate the release of an API from pharmaceutical formulations in the stomach [33,34]; therefore, an increase in the % HCTZ released at 30 min was observed with an increase in the Eud ® E100 content.…”