Novel glibenclamide–phospholipid complex for diabetic treatment: formulation, physicochemical characterization, and in-vivo evaluation
By: Rathor, Sandeep
.
Contributor(s): Bhatt, D.C.
Publisher: Karnataka Association of Pharmaceutical Teachers of India (APTI) 2022Edition: Vol.56(3), Jul-Sep.Description: 697-705p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical education and researchSummary: Introduction: Formulation of phospholipid complex is an ideal approach to improve the
solubility of poorly soluble drugs. Objectives: This study has been aimed to prepare a novel
glibenclamide-phospholipid complex by using the solvent evaporation technique. Materials
and Methods: Because glibenclamide is a weakly soluble medication, complexing it with
phospholipids is an excellent way to enhance its solubility. The phospholipid complex
of Glibenclamide was produced using the solvent-evaporation technique to enhance its
oral efficacy. The formulation was characterized and evaluated by various parameters
including FTIR, DSC, PXRD, SEM, TEM,
in vitro drug release, and
in vivo pharmacokinetic
studies in Wistar rats plasma. According to studies, the Glibenclamide phosphates
combination is significantly more water-soluble than the physical combination and pure
Glibenclamide. The oral bioavailability of the glibenclamide-phospholipids complex was
measured by using HPLC in Wistar rats’ plasma. Results: There was no substantial
interaction between the medication and the phospholipid in the formulation, according
to the FTIR and PXRD findings. The morphology of the formulation was verified by
SEM and TEM investigations, indicating that the crystalline form had been converted
to an amorphous form. The glibenclamide-phospholipids complex had a greater peak
plasma concentration (5.1 vs. 3.8 g/mL), its AUC was higher (14.65 vs. 11.81 μgh/L),
and its T1/2 was longer (2.4 vs. 3.1 hr), showing that it enhanced drug dissolution
rate. Conclusion: The findings showed that increasing the oral bioavailability of water-
insoluble medicines by phospholipid-complexation is a potential approach. The results
showed that phospholipid-complexation may be used to enhance the oral bioavailability
of water-insoluble drugs.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2022-1375 |
Introduction: Formulation of phospholipid complex is an ideal approach to improve the
solubility of poorly soluble drugs. Objectives: This study has been aimed to prepare a novel
glibenclamide-phospholipid complex by using the solvent evaporation technique. Materials
and Methods: Because glibenclamide is a weakly soluble medication, complexing it with
phospholipids is an excellent way to enhance its solubility. The phospholipid complex
of Glibenclamide was produced using the solvent-evaporation technique to enhance its
oral efficacy. The formulation was characterized and evaluated by various parameters
including FTIR, DSC, PXRD, SEM, TEM,
in vitro drug release, and
in vivo pharmacokinetic
studies in Wistar rats plasma. According to studies, the Glibenclamide phosphates
combination is significantly more water-soluble than the physical combination and pure
Glibenclamide. The oral bioavailability of the glibenclamide-phospholipids complex was
measured by using HPLC in Wistar rats’ plasma. Results: There was no substantial
interaction between the medication and the phospholipid in the formulation, according
to the FTIR and PXRD findings. The morphology of the formulation was verified by
SEM and TEM investigations, indicating that the crystalline form had been converted
to an amorphous form. The glibenclamide-phospholipids complex had a greater peak
plasma concentration (5.1 vs. 3.8 g/mL), its AUC was higher (14.65 vs. 11.81 μgh/L),
and its T1/2 was longer (2.4 vs. 3.1 hr), showing that it enhanced drug dissolution
rate. Conclusion: The findings showed that increasing the oral bioavailability of water-
insoluble medicines by phospholipid-complexation is a potential approach. The results
showed that phospholipid-complexation may be used to enhance the oral bioavailability
of water-insoluble drugs.
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