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Formulation and evaluation of metformin hydrochloride-loaded niosomes as controlled release drug delivery system
Open accessAbstract
Lactic acidosis is a serious, metabolic complication that may occur due to metformin hydrochloride (MH) accumulation during the treatment of diabetes mellitus. The aim of this study is to enhance the bioavailability of MH by oral route. Span 40 and cholesterol were used for the preparation of MH-loaded niosomes by the reverse phase evaporation technique. Dicetyl phosphate (DCP) and 1,2-dioleoyl-3-trimethylammonium-propane chloride salt (DOTAP) were used to obtain negatively and positively charged vesicles, respectively. The mean particle size ranged from 223.5 to 384.6 nm and the MH-loaded niosomes' surface was negatively charged in the absence of charge inducing agents (-16.6 ± 1.4 mV) and also with DCP (-26.9 ± 1.0 mV), while it was positively charged (+8.7 ± 1.2 mV) with DOTAP. High entrapment efficiency was observed in all the formulations. MH-loaded niosomes were found to effectively sustain the release of drug, particularly with positively charged niosomes. The bioavailability of MH-loaded niosomes was assessed by measuring the serum values of glucose and metformin in the different studied Wistar rats groups. The pharmacokinetic data of MH-loaded niosomal preparation showed a significant prolongation and increased intensity of hypoglycemic effect more than that observed for free MH solution. Area above the blood glucose levels-time curve (AAC), maximum hypoglycemic response and time of maximum response (T(max)) were significantly higher (p < 0.001) when MH was administered in niosomal form compared to free drug solution. It could be concluded that MH-loaded niosome is promising extended-release preparation with better hypoglycemic efficiency.
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“Pharmacokinetic testing confirmed the better efficacy of metformin-loaded niosomes over pure metformin in reducing blood glucose levels.84”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [84]
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Metadata
- Authors
- Hasan, A. A., Madkor, H., & Wageh, S.
- Affiliations
- Zagazig University (EG)
- Al-Azhar University (EG)
- Corresponding author
- Hasan, Azza A.
- ORCID
- Madkor, Hafez
- Venue
- Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2013-04
- Volume
- 20
- Issue
- 3-4
- Pages
- 120-126
- ISSN
- 1071-7544 (ISSN-L)
- 1521-0464
- OpenAlex
- W2163002418
- Cited by
- 122
- References
- 39
- Citations by year
- 2026: 3 · 2025: 17 · 2024: 7 · 2023: 16 · 2022: 16 · 2021: 8 · 2020: 12 · 2019: 12 · 2018: 8 · 2017: 9 · 2016: 4 · 2015: 7 · 2014: 3
- FWCI
- 2.81
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- metformin hydrochloride, niosomes, controlled release, oral drug delivery, bioavailability, diabetes mellitus, lactic acidosis, DOTAP, dicetyl phosphate, encapsulation efficiency, hypoglycemic effect, pharmacokinetics, Span 40, cholesterol
- MeSH terms
- Animals, Blood Glucose, Chemistry, Pharmaceutical, Delayed-Action Preparations, Drug Evaluation, Preclinical, Liposomes, Male, Metformin, Random Allocation, Drug Delivery Systems, Rats, Wistar, Rats
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