Enhanced oral absorption of insulin: hydrophobic ion pairing and a self-microemulsifying drug delivery system using a D-optimal mixture design

Goo, Yoon Tae; Lee, Sangkil; Choi, Ji Yeh; Kim, Min Song; Sin, Gi Hyeong; Hong, Sun Ho; Kim, Chang‐Hyun; Song, Seh Hyon; Choi, Young Wook

doi:10.1080/10717544.2022.2118399

Cited by 16 publications

(4 citation statements)

References 62 publications

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“…Scheffe’s mixture design was employed to examine the excipients percentages used with the drug in microemulsions formation toward its solubility, particle size, % transmittance, and % precipitation. As a result, the optimized formulation of ticagrelor in SMEDDS consisting of 10% Capmul MCM, 53.8% Cremophor EL, and 36.2% Transcutol P resulted in maximum values of solubility and % transmittance and minimum values of % precipitation and particle size, along with an exhibited oral bioavailability up to 637.1% as compared to the ticagrelor suspension [ 95 ].…”

Section: Advantages Of Applying Doe Techniques For the Development Of...mentioning

confidence: 99%

Application of Design of Experiments in the Development of Self-Microemulsifying Drug Delivery Systems

et al. 2023

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Oral delivery has become the route of choice among all other types of drug administrations. However, typical chronic disease drugs are often poorly water-soluble, have low dissolution rates, and undergo first-pass metabolism, ultimately leading to low bioavailability and lack of efficacy. The lipid-based formulation offers tremendous benefits of using versatile excipients and has great compatibility with all types of dosage forms. Self-microemulsifying drug delivery system (SMEDDS) promotes drug self-emulsification in a combination of oil, surfactant, and co-surfactant, thereby facilitating better drug solubility and absorption. The feasible preparation of SMEDDS creates a promising strategy to improve the drawbacks of lipophilic drugs administered orally. Selecting a decent mixing among these components is, therefore, of importance for successful SMEDDS. Quality by Design (QbD) brings a systematic approach to drug development, and it offers promise to significantly improve the manufacturing quality performance of SMEDDS. Furthermore, it could be benefited efficiently by conducting pre-formulation studies integrated with the statistical design of experiment (DoE). In this review, we highlight the recent findings for the development of microemulsions and SMEDDS by using DoE methods to optimize the formulations for drugs in different excipients with controllable ratios. A brief overview of DoE concepts is discussed, along with its technical benefits in improving SMEDDS formulations.

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Section: Advantages Of Applying Doe Techniques For the Development Of...mentioning

confidence: 99%

Application of Design of Experiments in the Development of Self-Microemulsifying Drug Delivery Systems

et al. 2023

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“…Stability of Ins-SDS loaded optimized SMEDDS against proteolytic degradation was investigated using simulated intestinal fluid (SIF) [ 10 ]. To prepare SIF, trypsin and chymotrypsin were added to the Tris buffer.…”

Section: Methodsmentioning

confidence: 99%

Design and Evaluation of Hydrophobic Ion Paired Insulin Loaded Self Micro-Emulsifying Drug Delivery System for Oral Delivery

et al. 2023

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Despite several novel and innovative approaches, clinical translation of oral insulin delivery into commercially viable treatment is still challenging due to its poor absorption and rapid degradation in GIT. Thus, an insulin-SDS hydrophobic ion pair loaded self-microemulsifying drug delivery system (SMEDDS) was formulated to exploit the hypoglycemic effects of orally delivered insulin. Insulin was initially hydrophobically ion paired with sodium dodecyl sulphate (SDS) to enhance its lipophilicity. The successful complexation of Insulin-SDS was confirmed by FTIR and surface morphology was evaluated using SEM. Stability of insulin after its release from HIP complex was evaluated using SDS PAGE. Subsequently, Ins-SDS loaded SMEDDS was optimized using two factorial designs. In vitro stability of insulin entrapped in optimized SMEDDS against proteolytic degradation was also assessed. Further, antidiabetic activity of optimized Ins-SDS loaded SMEDDS was evaluated in diabetic rats. Insulin complexed with SDS at 6:1 (SDS/insulin) molar ratio with almost five-fold increased lipophilicity. The SMEDDS was optimized at 10% Labraphil M2125 CS, 70% Cremophore EL, and 20% Transcutol HP with better proteolytic stability and oral antidiabetic activity. An Ins-SDS loaded SMEDDS was successfully optimized. Compared with insulin and Ins-SDS complex, the optimized SMEDDS displayed considerable resistance to GI enzymes. Thus, the SMEDDS showed potential for effective delivery of macromolecular drugs with improved oral bioavailability.

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“…( 2023 ). It is a polar hydrophilic peptide (Chen et al., 2018 ) with a log P value of −1.61 (Goo et al., 2022 ), and a melting point (m.p.) around 65 °C (stable zinc-INS hexamer has a m.p.…”

Section: Design Principles For Biodegradable/dissolvable Polymeric In...mentioning

confidence: 99%

Biodegradable polymeric insulin microneedles – a design and materials perspective review

Starlin Chellathurai,

Mahmood,

Mohamed Sofian

et al. 2023

Drug Delivery

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Microneedle (MN) delivery devices are more accepted by people than regular traditional needle injections (e.g. vaccination) due to their simplicity and adaptability. Thus, patients of chronic diseases like diabetes look for alternative pain-free treatment regimens circumventing regular subcutaneous injections. Insulin microneedles (INS-MNs) are a thoughtfully researched topic (1) to overcome needle phobia in patients, (2) for controlled delivery of the peptide, (3) decreasing the frequency of drug administration, (4) to ease the drug administration procedure, and (5) thus increasing patient adherence to the treatment dosage regimes. MNs physically disrupt the hard outer skin layer to create minuscule pores for insulin (INS) to pass through the dermal capillaries into the systemic circulation. Biodegradable polymeric MNs are of greater significance for INS and vaccine delivery than silicon, metal, glass, or non-biodegradable polymeric MNs due to their ease of fabrication, mass production, cost-effectiveness, and bioerodability. In recent years, INS-MNs have been researched to deliver INS through the transdermal implants, buccal mucosa, stomach wall, intestinal mucosal layers, and colonic mucosa apart from the usual transdermal delivery. This review focuses on the design characteristics and the applications of biodegradable/dissolvable polymeric INS-MNs in transdermal, intra-oral, gastrointestinal (GI), and implantable delivery. The prospective approaches to formulate safe, controlled-release INS-MNs were highlighted. Biodegradable/dissolvable polymers, their significance, their impact on MN morphology, and INS release characteristics were outlined. The developments in biodegradable polymeric INS-MN technology were briefly discussed. Bio-erodible polymer selection, MN fabrication and evaluation factors, and other design aspects were elaborated.

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Enhanced oral absorption of insulin: hydrophobic ion pairing and a self-microemulsifying drug delivery system using a D-optimal mixture design

Cited by 16 publications

References 62 publications

Application of Design of Experiments in the Development of Self-Microemulsifying Drug Delivery Systems

Application of Design of Experiments in the Development of Self-Microemulsifying Drug Delivery Systems

Design and Evaluation of Hydrophobic Ion Paired Insulin Loaded Self Micro-Emulsifying Drug Delivery System for Oral Delivery

Biodegradable polymeric insulin microneedles – a design and materials perspective review

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