Summary and future perspectives for oral insulin delivery

Sonia, Thundiparambil Azeez; Sharma, Chandra P.

doi:10.1533/9781908818683.311

Cited by 5 publications

(5 citation statements)

References 38 publications

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“…Hydrogels can swell and de‐swell in response to the body's fluctuating pH conditions and can control insulin release from the polymer matrix 173 . The physicochemical and biological stability of the entrapped insulin is improved by hydrogels comprised of mucoadhesive units, such as PMAA‐, MAA‐, and CS‐based polymeric systems 174 . For example, chitosan has pH‐responsive solubility, resulting in the formation of a thin film.…”

Section: Applications Of Polyelectrolytes In Drug Deliverymentioning

confidence: 99%

“…These liposomes release the drug into the small intestinal pH with additional protection from bile salts and proteolytic enzymes. The technology is in the development phase 156,174 …”

Section: Technologies Under Developmentmentioning

confidence: 99%

“…173 The physicochemical and biological stability of the entrapped insulin is improved by hydrogels comprised of mucoadhesive units, such as PMAA-, MAA-, and CS-based polymeric systems. 174 For example, chitosan has pH-responsive solubility, resulting in the formation of a thin film. Because of its high adhesiveness, CS can also adhere to the anionic mucosal layer of the intestinal wall, break down tight connections between epithelial cells, and aid in the extended-release of drugs that have been encapsulated.…”

Section: Targeted Delivery Of Insulinmentioning

confidence: 99%

“…The technology is in the development phase. 156,174 7 | RECENT PATENTS Some recent patents on the formulations based on pHresponsive delivery mechanisms are given in Table 8.…”

Section: Orasome™mentioning

confidence: 99%

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pH‐responsive polymers for drug delivery: Trends and opportunities

Singh,

Nayak

2023

Journal of Polymer Science

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Polymer science has applications in biomedical engineering, prosthetics, surgical implants, and prospective pharmaceutical excipients for drug delivery. “Intelligent or Smart Polymers” are created for drug targeting either by derivatization of natural polymers or controlled radical polymerization of electrolytes. Their mode of action is governed by the environmental stimuli viz. temperature, pH, ionic concentration, magnetism, and so on. pH‐responsive polymers, because of their self‐assembling behavior, alter their solubility, conformation, surface activity, and hydrophilicity when exposed to a specific pH. The physiological pH varies from acidic nuclei to alkaline cytoplasm and highly acidic gastric juice to slightly alkaline plasma; thus, various polymers are under study for delivering small molecules, genes, peptides, enzymes, growth factors, and antibodies. The non‐invasive drug delivery routes like oral, ocular, nasal, pulmonary, transdermal, and rectal routes can be explored for targeting recombinant proteins, monoclonal antibodies, and small molecules with particular emphasis on the individual's physiological and pathological state. Further, these polymers can be designed into various architectures like dendrimers, liposomes, micelles, and metallic nanoparticles that can serve as drug reservoirs for sustaining drug release. The challenges in this field are the selection of biocompatible polymers with ease of synthesis and scale‐up, ensuring effective drug‐loading, and stability aspects, producing robust pharmacological data, and timely regulatory approvals. This review exclusively explores the physicochemical characteristics of pH‐responsive polymers, their categorization, various architectural entities, recent studies and patents, and their emerging applications concerning specific diseases.

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Section: Applications Of Polyelectrolytes In Drug Deliverymentioning

confidence: 99%

“…These liposomes release the drug into the small intestinal pH with additional protection from bile salts and proteolytic enzymes. The technology is in the development phase 156,174 …”

Section: Technologies Under Developmentmentioning

confidence: 99%

Section: Targeted Delivery Of Insulinmentioning

confidence: 99%

“…The technology is in the development phase. 156,174 7 | RECENT PATENTS Some recent patents on the formulations based on pHresponsive delivery mechanisms are given in Table 8.…”

Section: Orasome™mentioning

confidence: 99%

See 2 more Smart Citations

pH‐responsive polymers for drug delivery: Trends and opportunities

Singh,

Nayak

2023

Journal of Polymer Science

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“…This is highlighted by the recent FDA approval of oral formulations of octreotide (Mycapssa®), semaglutide (Rybelsus®) and desmopressin (Minirin®). Another interesting therapeutic peptide that would greatly benefit from an oral approach to delivery is insulin, which has received considerable attentions for advancing novel approaches to peptide delivery [6][7][8][9]. While much of the focus during oral peptide development has been on the improvement of intestinal absorption and oral bioavailability, another major hurdle in the way of capitalising on the many advantages of peptide therapeutics that must be addressed is their poor physical and chemical stability.…”

Section: Introductionmentioning

confidence: 99%

Elucidating the Degradation Pathways of Human Insulin in the Solid State

Fagan,

Bateman,

O’Shea

et al. 2024

J. Anal. Test.

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While there have been significant advances in the development of peptide oral dosage forms in recent years, highlighted by the clinical and commercial success of approved peptides such as Rybelsus®, there remain several barriers in the way of broad range applicability of this approach to peptide delivery. One such barrier includes the poor physical and chemical stability inherent to their structures, which persists in the solid state although degradation typically occurs at different rates and via different pathways in comparison to the solution state. Using insulin as a model peptide, this work sought to contribute to the development of analytical techniques for investigating common insulin degradation pathways. Chemically denatured, deamidated and aggregated samples were prepared and used to benchmark circular dichroism spectroscopy, reverse phase HPLC and size exclusion chromatography methods for the investigation of unfolding, chemical modifications and covalent aggregation of the insulin molecule respectively. Solid state degraded samples were prepared by heating insulin powder at 60 °C and 75% relative humidity for 1, 3, 5 and 7 d, and the degradation profiles of the samples were evaluated and compared with those observed in solution. While no unfolding was observed to occur, significant deamidation and covalent aggregation were detected. Reductive disulfide bond cleavage using dithiothreitol allowed for separation of the insulin A- and B-chains, offering a facile yet novel means of assessing the mechanisms of deamidation and covalent aggregation occurring in the solid state.

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