Formulation, Statistical Optimization, and In Vivo Pharmacodynamics of Cydonia oblonga Mucilage/Alginate Mucoadhesive Microspheres for the Delivery of Metformin HCl

Abstract

In recent years, attention has shifted toward the utilization of natural polymers for encapsulation and sustained release of health-hazardous drugs. The purpose of this work is to define and assess the sustained delivery potential and mucoadhesive potential of a Cydonia oblonga mucilage (COM) and sodium alginate (Na-Alg)-constituting polymeric delivery carrier of antidiabetic drugs with a specific end goal to retain metformin HCl in the stomach while expanding the drug’s bioavailability. Metformin HCl was encapsulated in mucoadhesive microspheres by an ionic gelation method. Polymers with different combinations were tried, and the resulting mucoadhesive COM/Na-Alg microspheres were assessed for particle size (mm) PS/Y1, drug encapsulation efficiency DEE (%)/Y2, and in vitro percentage cumulative drug release R12h/Y3 using Drug Design Expert software version 10. The response surface methodology by a 32-central composite design predicted optimal synthesis parameters for the microspheres to be 295 mg for COM and 219 mg for Na-Alg. An optimized formulation was prepared under these conditions and used to evaluate the micrometric properties, morphology and structural characteristics, swelling behavior, in vitro drug release, and kinetics. Acute toxicity studies were carried out on blank COM/Na-Alg microspheres to deem them safe for in vivo studies. The DEE (%) was calculated to be 85.8 ± 1.67, whereas scanning electron microscopy (SEM) showed a coarse surface with characteristic wrinkles and cracks with an optical microscopic particle size of 0.96 ± 2.45. The ex vivo tests showed great mucoadhesive properties and good swelling behavior with pH-responsive drug release and a significant reduction in in vivo blood glucose levels. The results advocated the use of optimized microspheres to enhance the bioactivity with a possible dose reduction, making it less symptomatic, reducing the expense of the treatment, and subsequently facilitating better patient compliance.

Formulation and Characterization of Inter-Penetrating Network of Isabgol Husk Mucilage for Modified Release of Diclofenac Sodium

“…The FTIR evaluation was performed in scanning range of 4000-650 cm -1 for the characteristic peaks. 15…”

“…The images were captured at a magnification of 45X, 100X, 500X, and 1000X with a 20kv excitation voltage. 15,18 Powder X-ray Diffractometry…”

“…This study aimed to sustain the release of Diclofenac sodium by formulating IPN microspheres by emulsion cross-linking method using Isabgol husk mucilage and PVA. 15…”

Formulation and Evaluation of Xanthan Gum Microspheres for the Sustained Release of Metformin Hydrochloride

“…Hariyadi et al [ 24 ] resorted to an ionotropic gelation technique for the preparation of MTH-loaded alginate microspheres. Cydonia oblonga mucilage/alginate mucoadhesive microspheres were assessed by Noreen et al [ 25 ], as a potential sustained-release and mucoadhesive system to improve MTH bioavailability. However, very little work has been done on the microencapsulation of MTH using xanthan gum.…”

Tuning the Microstructures of Electrospray Multicore Alginate Microspheres for the Enhanced Delivery of Astaxanthin

“…Alginate microspheres have proved their advantages in the delivery of active substances, such as odor taste masking, sensitive ingredients protection, and controllable release of bioactive substances. 7 The calcium alginate network in alginate microspheres is an effective barrier that protects sensitive ingredients from degradation. For example, alginate microspheres were used to deliver betacyanins, which significantly improved the stability of betacyanins during storage.…”