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Formulation development, in-vitro and ex-vivo evaluation of dry adsorbed solid lipid nanoparticles: an approach of overcoming olanzapine drawbacks Cover

Formulation development, in-vitro and ex-vivo evaluation of dry adsorbed solid lipid nanoparticles: an approach of overcoming olanzapine drawbacks

Open Access
|Apr 2024

Figures & Tables

Figure 1.

Solubility of OLZ in (a) solid lipids; (b) surfactants [values expressed as mean ± SD (n=3)].
Solubility of OLZ in (a) solid lipids; (b) surfactants [values expressed as mean ± SD (n=3)].

Figure 2.

Percentage desorption of SLNs from DANs prepared with different adsorbents [Values expressed as mean ± SD (N=3)].
Percentage desorption of SLNs from DANs prepared with different adsorbents [Values expressed as mean ± SD (N=3)].

Figure 3.

In-vitro drug release study of OLZ Suspension, SLNs, DANs in (a) 0.1N HCL; (b) PBS pH 6.8; (c) PBS pH 7.4; and (d) three stage multimedia [Values expressed as mean ± SD (N=3)].
In-vitro drug release study of OLZ Suspension, SLNs, DANs in (a) 0.1N HCL; (b) PBS pH 6.8; (c) PBS pH 7.4; and (d) three stage multimedia [Values expressed as mean ± SD (N=3)].

Figure 4.

In-vitro drug release of OLZ SLNs DANs in PBS pH 7.4: (a) Zero order; (b) First order; (c) Higuchi and (d) Korsemeyer–Peppas model.
In-vitro drug release of OLZ SLNs DANs in PBS pH 7.4: (a) Zero order; (b) First order; (c) Higuchi and (d) Korsemeyer–Peppas model.

Figure 5.

(a) DSC thermogram of OLZ and OLZ SLNs; (b) XRD spectra of the OLZ, PRE, SLNs, adsorbents and DANs. Scanning electron microscopy (SEM)
(a) DSC thermogram of OLZ and OLZ SLNs; (b) XRD spectra of the OLZ, PRE, SLNs, adsorbents and DANs. Scanning electron microscopy (SEM)

Figure 6.

SEM of (a) OLZ SLNs; (b) adsorbents; (c) and (d) DANs of OLZ SLNs.
SEM of (a) OLZ SLNs; (b) adsorbents; (c) and (d) DANs of OLZ SLNs.

Figure 7.

Ex-vivo intestinal permeability of OLZ suspension and SLNs [through treated and untreated jejunum] [values expressed as mean ± SD (N=3)].
Ex-vivo intestinal permeability of OLZ suspension and SLNs [through treated and untreated jejunum] [values expressed as mean ± SD (N=3)].

Effect of ST on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant (0.2%w/v) 70:30VD (mL)ST (min)Particle size (nm)PdIEE(%)
F18PRE10KELP+T80105303.30.62954
F14PRE10KELP+T801010256.30.56359
F19PRE10KELP+T801015238.00.27467

Effect of LC on particle size, PDI and EE_

Batch No.SL: PRE (%w/v)OLZ (mg)Surfactant (0.2%w/v)VD (mL)ST (min)Particle size (nm)PdIEE(%)
F70.4510KELP1010247.10.32526
F10.5010KELP1010253.70.07649
F80.5510KELP1010267.30.49452

Effect of surfactant on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant (0.2%w/v)VD (mL)ST (min)Particle size (nm)PdIEE(%)
F1PRE10KELP1010253.70.07649
F10PRE10KRH401010298.00.41626
F11PRE10T801010647.10.30358
F12PRE10KELP+T801010288.50.41361

Effect of surfactant ratio on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant: KELP+T80 (0.2%w/v)VD (mL)ST (min)Particle size (nm)PdIEE(%)
F12PRE1050:501010288.50.41361
F13PRE1060:401010266.90.59659
F14PRE1070:301010256.30.56359
F15PRE1080:201010241.60.28351

Effect of SC on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant: KELP+T80 (70:30)VD (mL)ST (min)Particle size (nm)PdIEE(%)
F16PRE100.151010309.71.00063
F14PRE100.201010256.30.56359
F17PRE100.251010215.80.02648

Linearity and diffusion exponent from kinetic plots for different mediums used for in-vitro drug release study for OLZ SLNs DANs

MediaModel
Zero order (R2)First order (R2)Higuchi (R2)Korsemeyer–Peppas
R2Diffusion exponent (n)
0.1 N HCL0.4870.5850.6890.9860.415
PBS pH 6.80.8660.9400.9700.9840.434
PBS pH 7.40.8700.9590.9710.9850.481
Three stage multimedia0.4160.6400.9610.8370.264

Effect of DC on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant (0.2%w/v)VD (mL)ST (min)Particle size (nm)PdIEE(%)
F1PRE10KELP1010253.70.07649
F9PRE12.5KELP1010299.00.21753

Effect of STM on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant (0.2%w/v) 70:30VD (mL)ST (min)STMParticle size (nm)PdIEE(%)
F20PRE10KELP+T8010102-8285.80.42538
F19PRE10KELP+T801010RT238.00.27467

Screening of adsorbents_

AdsorbentMannitolLactoseKCLNUS2NUS2 + MannitolNUS2 + LactoseNUS2 + ACL
Particle size (nm)401.2308.4382.9364.8361.9463.3302.4
PdI0.4000.2980.4550.4100.5990.8520.494
HRPoorFairPassablePassableGoodGoodGood
CIPoorFairFairFairGoodGoodGood
Angle of reposeExcellentExcellentgoodExcellentExcellentExcellentExcellent
RemarksFungal growthParticles in the range of 5000 nm also presentRat Holing-Fungal growthParticles in the range of 5000 nm also present-

Effect of SL on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactant (0.2%w/v)VD (mL)ST (min)Particle size (nm)PdIEE (%)
F1PRE10KELP1010253.70.07649
F2GMS10KELP1010527.00.70954
F3CMPR10KELP1010630.01.00047
F4PRE + GMS10KELP1010328.20.31250
F5PRE+CMPR10KELP1010164.00.48240
F6GMS+CMPR10KELP1010719.30.20345

Effect of VD on particle size, PDI and EE_

Batch No.SL (0.5%w/v)OLZ (mg)Surfactants (0.2%w/v) 70:30VD (mL)ST (min)Particle size (nm)PdIEE(%)
F21PRE10KELP+T80510222.20.03131
F19PRE10KELP+T801010238.00.27467
Language: English
Page range: 1 - 15
Submitted on: Apr 5, 2023
Accepted on: Aug 29, 2023
Published on: Apr 20, 2024
Published by: Comenius University in Bratislava, Faculty of Pharmacy
In partnership with: Paradigm Publishing Services
Publication frequency: 2 issues per year
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© 2024 Rajashree Hirlekar, Alfiha Momin, Srinivas Bhairy, published by Comenius University in Bratislava, Faculty of Pharmacy
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.