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Abstract
Sitagliptin (MK–0431) is a widely and commonly used oral hypoglycemic drug in the treatment of type 2 diabetes mellitus; patients typically take higher doses of this drug (50 mg, twice daily). One drawback is that only 38% of the drug is bound reversibly to plasma proteins and 79% is excreted in urine without being metabolized. To overcome this issue, there is a need for a better drug-delivery method to improve its efficacy in patients. It has been found that in existing formulations, the drug content is 72.5% ± 5% and the percentage yield is 84.9% ± 3%. In this study, sitagliptin nanoparticles (sizes ranging from 210 to 618 nm) were developed. The bioadhesion properties of the nanoparticles, as well as the swelling of the nanoparticles on the mucus membrane aided in sustained drug release. The pattern of drug release was in accordance with the Peppas model. Fourier-transform infrared (FTIR) spectroscopy demonstrated that there were no significant interactions between sitagliptin and chitosan. Differential scanning calorimetry (DSC) results showed an absence of drug peaks due to the fact that the drug was present in an amorphous state. Mucoadhesive nanoparticles were formulated using sitagliptin and were effective for about 12 hours in the gastrointestinal tract. When compared to conventional sitagliptin administration, use of a nanoparticle delivery system demonstrated greater benefits for use in oral delivery applications. This is the first time that a drug-delivery method based on the mucoadhesive properties of nanoparticles could prolong the drug-release time of sitagliptin.
Highlights
Diabetes represents a complex set of health disorders that affect many patients irrespective of age
A total of 1,000 mg each of SCN and chitosan were taken and combined in 250 mL of deionized water. e solutions were made to a pH level of 5; acetic acid (0.25% [v/v]) was used to prepare the solution for spray drying. e spray-dried nanoparticles were developed using a spray dryer in a laboratory setting (Buchi B-90, Labortechnik AG, Flawil, Switzerland). e process set at an inlet temperature of 100°C with a rate of aspiration of 100%, a spray flow rate of 160 L/hour, and the pump was adjusted to 2.5 mL/minute
E developed nanoparticles demonstrated an almost spherical scattering pattern, which occurred in a rhythmic manner. ere was no evidence of any contractions on the surface (Figure 1(a)), and the nanoparticles were compared with the pure drug (Figure 1(b); sitagliptin) and polymer (Figure 1(c); chitosan)
Summary
Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics. One drawback is that only 38% of the drug is bound reversibly to plasma proteins and 79% is excreted in urine without being metabolized. To overcome this issue, there is a need for a better drug-delivery method to improve its efficacy in patients. Mucoadhesive nanoparticles were formulated using sitagliptin and were effective for about 12 hours in the gastrointestinal tract. Is is the first time that a drug-delivery method based on the mucoadhesive properties of nanoparticles could prolong the drug-release time of sitagliptin When compared to conventional sitagliptin administration, use of a nanoparticle delivery system demonstrated greater benefits for use in oral delivery applications. is is the first time that a drug-delivery method based on the mucoadhesive properties of nanoparticles could prolong the drug-release time of sitagliptin
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