Development and characterization of oral fast-dissolving strip incorporated with olmesartan medoxomil nanocrystals for solubility enhancement : Multilevel categoric optimization using DOE
By: Rajakumari, V
.
Contributor(s): Nithya, R.
Publisher: Mandsaur BRNSS Publication Hub. 2022Edition: Vol.16(2), Apr-Jun.Description: 172-182p.Subject(s): PHARMACEUTICSOnline resources: Click here to access online
In:
International journal of green pharmacySummary: Aim: Olmesartan medoxomil (OLM) is an antihypertensive drug available as an oral solid dosage form (tablet)
with a restricted bioavailability of 28.6%. This might be attributed due to the low solubility and low permeability
of the drug. The primary goal of this study was to enhance the solubility of OLM by formulating OLM nanocrystals
(NC) and incorporating them into Oral Fast-Dissolving Strips (OFDSs) that will be made available for geriatric
patients. Materials and Methods: Initially, nanosuspension (solvent-anti-solvent addition) was prepared using
different concentrations of stabilizers and characterized for particle size (PS), polydispersity index (PDI), and zeta
potential. Further, the nanosuspension was freeze-dried to obtain NC and it was characterized for crystallinity
and surface morphology. In addition, the OLM NCs were incorporated into OFDS (solvent evaporation
technique) and optimized by Multilevel Categoric design (24 × 2 2) using Design Expert® software. The OFDS
was evaluated for weight variation, thickness, tensile strength, drug content, disintegration time, and dissolution.
Results and Discussion: F30 shows PS, PDI, and zeta potential of 764.6 nm, 0.310, and −28.7 mV, respectively.
The DSC thermograms showed that the reduction in crystallinity of OLM NC compared to pure OLM and the
SEM images reveal rod-shaped crystals. The weight variation, thickness, surface pH, and drug content of OLM
loaded OFDS obtained satisfactory results. The disintegration time, folding endurance, and tensile strength of the
optimized formulation were found to be 20 ± 0.41 s, 125 ± 0.47 times, and 1328.8 ± 0.82 N/m, respectively. The
drug release from the formulation was found to be 85.28% at the end of 5 min; the drug release kinetics indicated
that it follows non-fickian diffusion and stability studies (25°C/60% RH) reveal that the formulation was stable.
Conclusion: The results conclude that NCs approach is a promising techniques to improve solubility of poorly
soluble drug.
Key words:
Design of experiment, nanocrystals, olmesartan medoxomil, oral fast-dissolving strip, solvent
evaporation, solvent-antisolvent addition
| Item type | Current location | Collection | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Reference | Not For Loan | 2022-1238 |
Aim: Olmesartan medoxomil (OLM) is an antihypertensive drug available as an oral solid dosage form (tablet)
with a restricted bioavailability of 28.6%. This might be attributed due to the low solubility and low permeability
of the drug. The primary goal of this study was to enhance the solubility of OLM by formulating OLM nanocrystals
(NC) and incorporating them into Oral Fast-Dissolving Strips (OFDSs) that will be made available for geriatric
patients. Materials and Methods: Initially, nanosuspension (solvent-anti-solvent addition) was prepared using
different concentrations of stabilizers and characterized for particle size (PS), polydispersity index (PDI), and zeta
potential. Further, the nanosuspension was freeze-dried to obtain NC and it was characterized for crystallinity
and surface morphology. In addition, the OLM NCs were incorporated into OFDS (solvent evaporation
technique) and optimized by Multilevel Categoric design (24 × 2 2) using Design Expert® software. The OFDS
was evaluated for weight variation, thickness, tensile strength, drug content, disintegration time, and dissolution.
Results and Discussion: F30 shows PS, PDI, and zeta potential of 764.6 nm, 0.310, and −28.7 mV, respectively.
The DSC thermograms showed that the reduction in crystallinity of OLM NC compared to pure OLM and the
SEM images reveal rod-shaped crystals. The weight variation, thickness, surface pH, and drug content of OLM
loaded OFDS obtained satisfactory results. The disintegration time, folding endurance, and tensile strength of the
optimized formulation were found to be 20 ± 0.41 s, 125 ± 0.47 times, and 1328.8 ± 0.82 N/m, respectively. The
drug release from the formulation was found to be 85.28% at the end of 5 min; the drug release kinetics indicated
that it follows non-fickian diffusion and stability studies (25°C/60% RH) reveal that the formulation was stable.
Conclusion: The results conclude that NCs approach is a promising techniques to improve solubility of poorly
soluble drug.
Key words:
Design of experiment, nanocrystals, olmesartan medoxomil, oral fast-dissolving strip, solvent
evaporation, solvent-antisolvent addition
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