Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics
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 uri...
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doaj-cb78a62267c14286b6e4d4b0f434737e2020-11-25T02:31:46ZengHindawi LimitedBioMed Research International2314-61332314-61412019-01-01201910.1155/2019/39509423950942Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of DiabeticsNagaraja SreeHarsha0Chandramouli Ramnarayanan1Bandar E. Al-Dhubiab2Anroop B. Nair3Jagadeesh G. Hiremath4Katharigatta N. Venugopala5Roopashree T. Satish6Mahesh Attimarad7Arshia Shariff8Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi ArabiaDepartment of Quality Assurance, Krupanidhi College of Pharmacy, Bengaluru, IndiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi ArabiaDepartment of Pharmaceutics, Vidya Siri College of Pharmacy, Bengaluru, IndiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi ArabiaDepartment of Pharmacognosy, Government College of Pharmacy, Bengaluru, IndiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi ArabiaDepartment of Pharmaceutics, Alard College of Pharmacy, Savitribai Phule, Pune University, Pune, IndiaSitagliptin (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.http://dx.doi.org/10.1155/2019/3950942 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Nagaraja SreeHarsha Chandramouli Ramnarayanan Bandar E. Al-Dhubiab Anroop B. Nair Jagadeesh G. Hiremath Katharigatta N. Venugopala Roopashree T. Satish Mahesh Attimarad Arshia Shariff |
spellingShingle |
Nagaraja SreeHarsha Chandramouli Ramnarayanan Bandar E. Al-Dhubiab Anroop B. Nair Jagadeesh G. Hiremath Katharigatta N. Venugopala Roopashree T. Satish Mahesh Attimarad Arshia Shariff Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics BioMed Research International |
author_facet |
Nagaraja SreeHarsha Chandramouli Ramnarayanan Bandar E. Al-Dhubiab Anroop B. Nair Jagadeesh G. Hiremath Katharigatta N. Venugopala Roopashree T. Satish Mahesh Attimarad Arshia Shariff |
author_sort |
Nagaraja SreeHarsha |
title |
Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics |
title_short |
Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics |
title_full |
Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics |
title_fullStr |
Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics |
title_full_unstemmed |
Mucoadhesive Particles: A Novel, Prolonged-Release Nanocarrier of Sitagliptin for the Treatment of Diabetics |
title_sort |
mucoadhesive particles: a novel, prolonged-release nanocarrier of sitagliptin for the treatment of diabetics |
publisher |
Hindawi Limited |
series |
BioMed Research International |
issn |
2314-6133 2314-6141 |
publishDate |
2019-01-01 |
description |
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. |
url |
http://dx.doi.org/10.1155/2019/3950942 |
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