Formulation, physicochemical characterization and in vitro evaluation of human insulin-loaded microspheres as potential oral carrier

Abstract

The objective of the present investigation was to formulate and characterize the human insulin entrapped Eudragit S100 microspheres containing protease inhibitors and to develop an optimized formulation with desirable features. A w/o/w multiple emulsion solvent evaporation technique was employed to produce microspheres of human insulin using Eudragit S-100 as coating material and polyvinyl alcohol as a stabilizer. The resultant microspheres were evaluated for drug-excipient compatibility, encapsulation efficiency, particle size, surface morphology, micromeritic properties, enteric nature, and in vitro drug release studies. Micromeritic properties indicated good flow properties and compressibility. In present investigation formulation F6 with drug/polymer ratio (1:100) was found to be optimal in terms of evaluated parameters where it showed a significantly higher percentage of encapsulation efficiency (76.84%) with minimal drug release (3.25%) in an acidic environment. The optimized formulation (F6) also possessed good spherical shape and particle size (57.42 µm) required to achieve the desired in vitro drug release profile at pH 7.4. The results confirmed that human insulin-loaded Eudragit S-100 microspheres containing protease inhibitor possessed good encapsulation efficiency, pH dependant controlled release carrying encapsulated insulin to its optimum site of absorption. This ultimately resulted in enhanced insulin absorption and biological response.Graphical Abstract

Development and Characterization of Novel Herbal Formulation (Polymeric Microspheres) of Syzygium Cumini Seed Extract

“…The micromeritic properties of all the formulations indicated that microspheres were free flowing in nature. The similar finding was also reported previously [9,16]. Data represent mean±standard deviation (SD), n=3.…”

“…It decreased when the external aqueous phase volume increased. When the stirring rate was increased from 800 to 1000 rpm, % yield increased (52.23-54.75%), but on further increase in the rate to 1500 rpm, it decreased [16,17].…”

Influences of different Fe sources on Fe bioavailability and homeostasis in SD rats

“…It can be seen that the relative bioavailability of enteric-coated Fe-Gly(1:1) and enteric-coated Fe-Gly(2:1) were higher than other iron supplements, indicating that the enteric coating increases the relative bioavailability of iron. The enteric coated insulin can reach the optimal absorption point for release and improve its absorption and utilization rate (Agrawal, Wakte, & Shelke, 2017); and after the nanoparticles are coated with the enteric coating, the unexpected degradation can be avoided, thereby improving the bioavailability (Öztürk, Mashal, Yegin, & Çalış, 2017); Clothing can further enhance the bioavailability of the drug by improving the stability of the drug (Petry, Löbmann, Grohganz, Rades, & Leopold, 2017). Therefore, when the amount of enteric-coated Fe-Gly(1:1) or enteric-coated Fe-Gly(2:1) is only 2/3 of ferrous sulfate in the diet, the equivalent iron supplement effect can be achieved, and this will reduce environmental pollution.…”

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“…[13] Micromeritics properties evaluation of microspheres was important to estimate the flow properties, packing properties, and porosity of powder, to determine their suitability for product formation. [14] The antibacterial activity is important to test because this parameter is directly proportional to concentration at the target site. [15] The authors were aimed to study the development of ciprofloxacin HCl-loaded alginate microspheres for direct delivery into lungs.…”