Abstract
Objective: Insulin is used to manage diabetes mellitus by subcutaneous injections regulary, that has become a part of patients life and is distressing for patients. Hence, we anticipate to get rid of the usage of subcutaneous injections completely from the medicine world and would make the diabetic people to say as “farewell to painful injections.”
 Methods: Virtual screening method (for selection of carriers), Toxtree tool (for toxicity evaluation of carriers), and discovery studio tool (for pharmacophore designing, absorption, distribution, metabolism, excretion, and toxicity [ADMET] analysis, designing oral insulin conjugates (OICs), and interaction studies between insulin receptor and OICs) were used for proposed study.
 Results: We have screened 14 competent drug delivering molecules (DDMs) from seven chemical compound databases. The ADMET and pharmacophoric properties of DDMs were analyzed by drug-informatics’ tools. Consequently, the DDMs were mono, di, and poly conjugated by covalent bonding with various binding sites of monomeric and hexameric form of human insulin and insulin-lispro (Humalog®) individually; and novel OICs were generated. Its binding efficiency and biological activity with insulin-receptor were determined.
 Conclusion: Inulin and Vitamin-B1 are the novel, safe, and proficient carriers for oral delivery of insulin. Insulin lispro is the remarkable option for oral delivery than other insulin forms.
Highlights
Drug discovery is an expensive but essential process which leads to innovation of therapeutic molecules to manage or cure diverse ailments of human beings through various modes of administration [1]
We report and analyze the structural series of novel drug delivering molecules (DDMs) and oral insulin conjugates (OICs) by drug-informatics
Carrier compounds were retrieved by the search terms of “Polymer” and “Biopolymer.” The compounds were filtered through literature analysis from the previous studies and virtual screening using a defined criteria listed below, in part akin to the Lipinski’s rule [11]; the DDMs should be: (a) Mono-disperse, (b) short-chain, (c) biocompatible, (d) lipophilic, (e) physically stability against gastric acids and proteolytic enzymes, (f) inert, and (g) non-toxic
Summary
Drug discovery is an expensive but essential process which leads to innovation of therapeutic molecules to manage or cure diverse ailments of human beings through various modes of administration [1] Some peculiar drugs such as proteins, hormones, enzymes, and peptides require efficient drug delivering molecules (DDMs) especially for oral formulations to reach therapeutic targets against the interruption of biological barriers. Numerous protein and hormone drugs are administered through various modes of painful injections which are making “fear of pain” among patients [3] In this case, the subcutaneous injection of insulin formulations has been the core therapy utilized for the management of the major global health threat of type 1 diabetes as well as type 2 diabetes since insulin’s discovery over 85 years ago [2]. Subcutaneously administered insulin is absorbed directly into the peripheral circulation without initial hepatic circulation, thereby exposing peripheral targets to higher insulin concentrations relative to the liver [3]
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