Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

Abstract

IntroductionIn previous studies, we successfully designed complex multicompartmental microcapsules as a platform for the oral targeted delivery of lipophilic drugs in type 2 diabetes (T2D). Probucol (PB) is an antihyperlipidemic and antioxidant drug with the potential to show benefits in T2D. We aimed to create a novel microencapsulated formulation of PB and to examine the shape, size, and chemical, thermal, and rheological properties of these microcapsules in vitro.MethodMicroencapsulation was carried out using the Büchi-based microencapsulating system developed in our laboratory. Using the polymer, sodium alginate (SA), empty (control, SA) and loaded (test, PB-SA) microcapsules were prepared at a constant ratio (1:30). Complete characterizations of microcapsules, in terms of morphology, thermal profiles, dispersity, and spectral studies, were carried out in triplicate.ResultsPB-SA microcapsules displayed uniform and homogeneous characteristics with an average diameter of 1 mm. The microcapsules exhibited pseudoplastic-thixotropic characteristics and showed no chemical interactions between the ingredients. These data were further supported by differential scanning calorimetric analysis and Fourier transform infrared spectral studies, suggesting microcapsule stability.ConclusionThe new PB-SA microcapsules have good structural properties and may be suitable for the oral delivery of PB in T2D. Further studies are required to examine the clinical efficacy and safety of PB in T2D.

Pharmacological and Biological Study of Microencapsulated Probucol-Secondary Bile Acid in a Diseased Mouse Model

“…This can act as a membrane-stabilising and structural support agent to increase the solubility and permeation of drugs [ 39 ]. These results support previous studies showing that bile acid incorporation did not change the shape and size but does alter the outer membrane and the internal complexity [ 27 , 38 ].…”

“…F1 as formulation-1 (PB-SA) and F2 as formulation-2 (PB-LCA-SA) microcapsules were prepared from the stock solutions as per our well-established laboratory method using the Ionic Gelation Vibrational Jet Flow Technology on a Büchi encapsulator (Büchi Labortechnik, Flawil, Switzerland) [ 26 , 27 , 28 , 29 , 30 , 31 , 32 ]. Briefly, different parameters were set in a frequency range of 1000–2000 Hz with a flow rate of 6 mL/min with a constant air pressure of 300 mbar.…”

“…Group 1 was orally gavaged with empty microcapsules, group 2 with free PB (powder) (PB: 80 mg/kg/day), group 3 with PB microcapsules (PB: 80 mg/kg/day), and group 4 with PB-LCA microcapsules (PB: 80 mg/kg/day and LCA: 40 mg/kg/day). The dosage of microcapsules was calculated according to our previous studies [ 27 , 49 ].…”

Functional Ingredients based on Nutritional Phenolics. A Case Study against Inflammation: Lippia Genus

“…On the other hand, secondary metabolites are a heterogeneous group of compounds that are found in specialized cells and they take action in secondary functions such as reproduction, protecting from predators or ultraviolet radiation, or producing sensory and colorimetric characteristics in different fruits, vegetables, and flowers [7,8]. In addition to these secondary metabolites being the focus of many studies in previous decades, especially phenolic compounds, they have also been shown to possess the ability to improve several physiological functions due to their anti-inflammatory, antimicrobial, antioxidant or cardioprotective properties [3,4,5,6].…”

“…For this reason, different extraction and isolation procedures have been developed to retrieve the responsible compounds from natural sources in order to reduce the necessary amounts of food that provide the desired beneficial effect. Moreover, different encapsulation methods have been implemented in order to increase the bioavailability of some phenolics with the aim of developing high value products such as functional foods or nutraceuticals [5,6]. These new products could help to reduce the prevalence of certain diseases or could even be used as a therapeutic alternative for the treatment of various ailments.…”