Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer

Abstract

The success of mucoadhesive drug delivery systems relies on the type of polymer used, which becomes adhesive naturally upon hydration. Intended polymers should be able to maintain prolonged contact with biological membranes, and to protect or cater the drug to a prolonged period. Most of the hydro polymers form weak non-covalent bonds, that hinder localization of dosage forms at specific sites resulting in therapeutic inefficiency. This can be overcome by the thiol functionalization of natural polymers. In the present study, natural okra gum (OG) was extracted, followed by thiolation (TOG) and evaluated for mucoadhesion property and its role in enhancing the efficacy of repaglinide as a model drug (short-acting Type II antidiabetic drug). The thiol functionalization of OG (TOG) was confirmed by a Fourier-transform infrared spectroscopy (FTIR) study that showed a polyhedral to a spherical shape that had a rougher surface. Differential scanning calorimetry (DSC) and X-Ray Diffraction (XRD) studies of TOG indicated a decline in endothermic transition temperature and high crystallinity, respectively, in comparison to OG. CSFR (Crushing Strength: Friability Ratio), weight and thickness variations of repaglinidetablets formulated using TOG were >80% and <2.5% respectively. The highest swelling index (107.89 ± 1.99%) and strong mucoadhesion due to high disulfide bonds were observed for repaglinide TOG tablets in comparison to RG OG tablets. In-vitro release studies indicated a controlled drug release from thiolated formulations proportional to the concentration of thiomers that have a good correlation with in-vivo studies. Pharmacokinetic studies indicated higher AUC (area under the curve), longer t 1/2 with thiomers. and Level A IVIV (in vitro in vivo) correlation was established from the bioavailability and dissolution data. Consequently, all the obtained results suggest that thiomers based formulations can be promising drug delivery systems, even in targeting onerous mucosal surfaces like nasal, ocular or vaginal.by suitable approaches such as thiolation, to employ in mucoadhesion drug delivery systems [9]. Nevertheless, to date, there has been no research reported in demonstrating the synthesis of thiolated okra gum (TOG) and evaluating its use in designing mucoadhesive drug delivery systems.The term bio adhesion depicts the adhesion of the polymer to the biological membrane. Specifically, when the adhesion is limited to the mucosal surface it is named mucoadhesion [10]. The conception of mucoadhesion, as well as mucoadhesion polymers, was developed in the mid 1980s as an intriguing methodology especially for targeting the delivery of drugs at a site or at the absorption window. Mucoadhesive polymers become adhesive on hydration and characterized to have prolonged contact and residence time with the mucous membrane. [11]. Despite a few notable exceptions, gastric mucoadhesive systems do not reach their full potential. The success of the majority of the first generation mucoadhesion polymers was limited owing to thei...

Thiolation of Biopolymers for Developing Drug Delivery Systems with Enhanced Mechanical and Mucoadhesive Properties: A Review

“…Naveen et al performed thiolation of okra gum for developing mucoadhesive tablets of repaglinide. Enhanced swelling, mucoadhesive strength and sustained drug release was reported in the study [ 110 ].…”

Assessing the Role of Artificial Intelligence in the Design of Drug Delivery Systems

“…The calculations, ability of reading, and impersonal use of records must be made noticeable, and every consequence should be examined for impersonal aptness. Our category has changed in such a way as executed in figure 1.voltaic pharma or health documents are important weapons for customized medicine and early observation and spot line cancellation, again to improve their impersonal worth and reduce fitness amounts [55][56][57][58][59][60][61][62][63]. The next effective implementation of AI in medicine is the use of software robots, as sensitivity training incarnation for preparation of Proliposomes, Microparticles, Solid lipid Nanoparticles, Nanoparticles, Nanoemulsion, Nanocrystals, Nanowires [64][65][66][67][68][69][70][71][72][73][74][75].…”

Clinical implications of novel polymer and lipid based drug delivery systems

“…Okra thioglycolic acid is used as a mucoadhesive polymer and is multifunctional. [42] Chitosan a naturally obtained polymer is also proven to be effective in weight loss. [43] Clinical implications by using lipid/ polymer drug delivery systems Although Lipid and Polymeric drug delivery systems are considered as one of the greatest advancements in the past decade there are many challenges when it comes to real-time clinical setting.…”