“…It was assumed that adding an additional layer to the formulation should affect the release rate of the films, but the order of release and the relations between profiles should remain similar to that of the monolayer films. The HPC polymer used in the second layer is a water-soluble polymer and its release rate is lower than that of Na-alginate [ 38 ]. The HPC polymer was selected because it dissolves more slowly than the main polymer, acts sufficiently as a barrier and can dissolve completely in the mouth.…”
The objective of this study was to develop buccal film formulations containing metoclopramide hydrochloride monohydrate (MCP) with and without a backing layer and to evaluate their release properties and physiochemical stability. The crystallization of MCP in the polymer matrix was monitored with image analysis techniques for rapid and scalable observation. The results showed that the addition of a protective layer and its thickness significantly affected the release rate and crystallization behavior of MCP in the formulations. The crystallization of MCP increased over time, and certain formulations showed higher susceptibility to crystallization. To understand the factors affecting the crystallization of MCP, the relationship between the viscosity and pH of the casting solution was examined, but no significant correlation was found. A significant correlation was observed between the plasticizer concentration and the physical state of MCP. Through a systematic Design of Experiment (DOE) approach, an optimal formulation was devised, successfully preventing crystallization of the active ingredient. However, enhancing the overall chemical stability of the formulated product remains a challenge.
“…It was assumed that adding an additional layer to the formulation should affect the release rate of the films, but the order of release and the relations between profiles should remain similar to that of the monolayer films. The HPC polymer used in the second layer is a water-soluble polymer and its release rate is lower than that of Na-alginate [ 38 ]. The HPC polymer was selected because it dissolves more slowly than the main polymer, acts sufficiently as a barrier and can dissolve completely in the mouth.…”
The objective of this study was to develop buccal film formulations containing metoclopramide hydrochloride monohydrate (MCP) with and without a backing layer and to evaluate their release properties and physiochemical stability. The crystallization of MCP in the polymer matrix was monitored with image analysis techniques for rapid and scalable observation. The results showed that the addition of a protective layer and its thickness significantly affected the release rate and crystallization behavior of MCP in the formulations. The crystallization of MCP increased over time, and certain formulations showed higher susceptibility to crystallization. To understand the factors affecting the crystallization of MCP, the relationship between the viscosity and pH of the casting solution was examined, but no significant correlation was found. A significant correlation was observed between the plasticizer concentration and the physical state of MCP. Through a systematic Design of Experiment (DOE) approach, an optimal formulation was devised, successfully preventing crystallization of the active ingredient. However, enhancing the overall chemical stability of the formulated product remains a challenge.
“…It shows 9.09% swelling in 0.1 N HCl (pH 1.2) after 2 h, 20% in phosphate buffer (pH 6.8) after 5 h, and 33.33% in phosphate buffer (pH 7.4) after 24 h, which was composed of sodium alginate 21 % and HPMC K4M 20%. These findings showed that the swelling index increased when HPMC K4M and SA concentrations were increased, forming a more compact structure of the hydrated gel layer that prevented the penetration of fluids [ 41 ]. Fig.…”
“…Pellets coated with a thin gold layer were examined via scanning electron microscopy (SEM; HITACHI-S3400N, Japan) to analyse shape and surface morphology. 23 …”
Purpose
The effective treatment of ulcerative colitis (UC) poses substantial challenges, and the aetiopathogenesis of UC is closely related to infectious, immunological and environmental factors. Currently, there is a considerable need for the development of orally bioavailable dosage forms that enable the effective delivery of therapeutic drugs to local diseased lesions in the gastrointestinal tract.
Methods
Berberine (BBR) and
Atractylodes macrocephala
Koidz (AM) volatile oil, derived from the Chinese herbs
Coptis chinensis
Franch and
Atractylodes macrocephala
Koidz, have anti-inflammatory and immunomodulatory activities. In this study, we prepared colon-targeted pellets loaded with BBR and stomach-targeted pellets loaded with AM volatile oil for the synergistic treatment of UC. The Box–Behnken design and β-cyclodextrin inclusion technique were used to optimize the enteric coating formula and prepare volatile oil inclusion compounds.
Results
The two types of pellets were spherical and had satisfactory physical properties. The pharmacokinetic results showed that the AUC and MRT values of the dual-targeted (DPs) pellets were higher than those of the control pellets. In addition, in vivo animal imaging confirmed that the DPs could effectively deliver BBR to the colon. Moreover, compared with sulfasalazine and monotherapy, DPs exerted a more significant anti-inflammatory effect by inhibiting the expression of inflammatory factors including IL-1β, IL-4, IL-6, TNF-α and MPO both in serum and tissues and enhancing immunity by decreasing the production of IgA and IgG.
Conclusion
The DPs play a synergistic anti-UC effect by exerting systemic and local anti-inflammatory and provide an effective oral targeted preparation for the treatment of UC.
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