The influence of the degree of esterification on the release characteristics ofin situgelling pectin formulations for oral sustained delivery of paracetamol

Miyazaki, Shôzo; Murofushi, Hanae; Shimoyama, Tetsuya; Itoh, Ken; Kobayashi, Mariko; Attwood, David

doi:10.3109/10837450.2011.653816

Cited by 4 publications

(4 citation statements)

References 15 publications

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“…In this experiment, the histamine H 2 -receptor antagonist famotidine (15 mg/kg) was injected intraperitoneally in mice 30 min before oral administration of insulin and penetratin. 16) As shown in Fig. 6, we confirmed that the pH of the gastric fluid of mice receiving famotidine was neutralized and modified pH could be maintained for at least 30 min.…”

Section: Exploring Optimized Doses Of Insulin Based On Spr Analysis Asupporting

confidence: 62%

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Exploration of the Key Factors for Optimizing the in Vivo Oral Delivery of Insulin by Using a Noncovalent Strategy with Cell-Penetrating Peptides

Kamei

Shigei

Hasegawa

et al. 2018

Biological & Pharmaceutical Bulletin

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This present study aimed to determine the optimal oral insulin delivery conditions that would maximize the utility of cell-penetrating peptides (CPPs) by using a noncovalent strategy. We first compared the effectiveness of two potential CPPs, penetratin and its analog PenetraMax, as absorption enhancers for insulin. The combined effect was evaluated under in vivo oral administration conditions. Both D-forms of CPPs were highly effective for increasing the oral absorption of insulin, and D-PenetraMax showed a more rapid onset of absorption enhancement effects compared with those of D-penetratin. However, synergistic absorption enhancement effects after combination treatment were not observed. Next, we tried a theoretical approach to establish optimized oral insulin delivery conditions. A surface plasmon resonance (SPR)-based analysis demonstrated that binding between insulin and penetratin (2 mM) might be saturated at 100-500 µM penetratin, while the bound concentration of penetratin could increase in accordance with an increased concentration of mixed insulin. To test this hypothesis, we investigated the effectiveness of different insulin doses in the gastric pH-neutralized mice. The results showed that the dissociation of noncovalent complexes of insulin and CPPs at the low gastric pH was prevented in these mice. Our findings clearly suggested that a noncovalent strategy with CPPs represents an effective approach for the L-form of CPP to increase the concentration of CPP-bound insulin to attain greater absorption of insulin, although this approach may not be appropriate for the D-form of CPP. Our findings will contribute to the development of oral dosage forms of insulin for noncovalent strategies involving CPP. Key words oral delivery; insulin; cell-penetrating peptide; penetratin; intermolecular interactionInsulin is the most important therapeutic agent for diabetes, even though there are now many other oral antidiabetic medicines available. Therefore, many types of insulin formulations, including rapid-and long-acting insulin as well as mixed type insulin, have been developed to date. 1-3) Diabetes patients can appropriately choose injectable types of insulin formulations; however, more convenient forms of insulin that can be administered via noninvasive routes, such as oral administration, have not yet been developed because of poor absorption through mucosal regions. [4][5][6][7] To further improve the QOL and compliance of patients, we aimed to develop a noninvasive form of insulin by using pharmaceutical technologies and drug delivery systems. Moreover, the oral route of insulin absorption has another advantage as insulin absorbed from the intestine first passes through the liver, similarly to endogenous insulin secreted to the portal vein; therefore, oral insulin can circumvent the risk of hypoglycemia.A major hurdle in the development of formulations for administration via noninvasive routes is the digestion and degradation in the harsh gastrointestinal environment. To protect biologics, such as insuli...

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Section: Exploring Optimized Doses Of Insulin Based On Spr Analysis Asupporting

confidence: 62%

“…1B. 16) In a preliminary experiment, the pH of gastric fluid was checked using universal pH indicator paper (Macherey-Nagel GmbH & Co., KG, Düren, Germany) before and after the oral dosing of PBS or the intraperitoneal (i.p.) injection of famotidine.…”

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confidence: 99%

Exploration of the Key Factors for Optimizing the in Vivo Oral Delivery of Insulin by Using a Noncovalent Strategy with Cell-Penetrating Peptides

Kamei

Shigei

Hasegawa

et al. 2018

Biological & Pharmaceutical Bulletin

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“…The potential applications of pectin with DE9 as a formulation with a degree of esterification (DE) of 9%, and DE31 as a formulation with a degree of esterification of 31%, were demonstrated as sustaining the floating of paracetamol with further in situ gelation in the stomach of gastric acidity-controlled rats with variety of pH (1.2–6.8) [128]. A substantial distinction regarding the in vivo gelling characteristics of the pectin DE9 and DE31 patterns was revealed by testing the stomach contents of gastric acidity-controlled rats at high pH intervals, following the oral administration of 1.5% ( w / v ) pectin sols.…”

Section: Pectin As Carriers For Drug Deliverymentioning

confidence: 99%

“…A substantial distinction regarding the in vivo gelling characteristics of the pectin DE9 and DE31 patterns was revealed by testing the stomach contents of gastric acidity-controlled rats at high pH intervals, following the oral administration of 1.5% ( w / v ) pectin sols. The significant gastric acidity influenced the decrease of the DE31 effectiveness, in comparison with compositions produced from pectin with DE9, and the stomach pH surged to 5.5 [128].…”

Section: Pectin As Carriers For Drug Deliverymentioning

confidence: 99%

Biological Activity and Pharmacological Application of Pectic Polysaccharides: A Review

et al. 2018

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Pectin is a polymer with a core of alternating α-1,4-linked d-galacturonic acid and α-1,2-l-rhamnose units, as well as a variety of neutral sugars such as arabinose, galactose, and lesser amounts of other sugars. Currently, native pectins have been compared to modified ones due to the development of natural medicines and health products. In this review, the results of a study of the bioactivity of pectic polysaccharides, including its various pharmacological applications, such as its immunoregulatory, anti-inflammatory, hypoglycemic, antibacterial, antioxidant and antitumor activities, have been summarized. The potential of pectins to contribute to the enhancement of drug delivery systems has been observed.

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Applications of polysaccharides in enzyme-triggered oral colon-specific drug delivery systems: A review

Gong,

Liu,

Wang

et al. 2024

International Journal of Biological Macromolecules

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The influence of the degree of esterification on the release characteristics ofin situgelling pectin formulations for oral sustained delivery of paracetamol

Cited by 4 publications

References 15 publications

Exploration of the Key Factors for Optimizing the <i>in Vivo</i> Oral Delivery of Insulin by Using a Noncovalent Strategy with Cell-Penetrating Peptides

Exploration of the Key Factors for Optimizing the <i>in Vivo</i> Oral Delivery of Insulin by Using a Noncovalent Strategy with Cell-Penetrating Peptides

Biological Activity and Pharmacological Application of Pectic Polysaccharides: A Review

Applications of polysaccharides in enzyme-triggered oral colon-specific drug delivery systems: A review

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