Accès libre

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

Rajashree Hirlekar
Rajashree Hirlekar
, 
Alfiha Momin
Alfiha Momin
 et 
Srinivas Bhairy
Srinivas Bhairy
   | 20 avr. 2024
European Pharmaceutical Journal's Cover Image
À propos de cet article
Article précédent
Article suivant
Citez
Article Category: Research paper
Publié en ligne: 20 avr. 2024
Pages: -
Reçu: 05 avr. 2023
Accepté: 29 août 2023
DOI: https://doi.org/10.2478/afpuc-2024-0004
Mots clés
© 2024 Rajashree Hirlekar et al., published by Sciendo
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

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) 70:30 VD (mL) ST (min) Particle size (nm) PdI EE(%)
F18 PRE 10 KELP+T80 10 5 303.3 0.629 54
F14 PRE 10 KELP+T80 10 10 256.3 0.563 59
F19 PRE 10 KELP+T80 10 15 238.0 0.274 67

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) PdI EE(%)
F7 0.45 10 KELP 10 10 247.1 0.325 26
F1 0.50 10 KELP 10 10 253.7 0.076 49
F8 0.55 10 KELP 10 10 267.3 0.494 52

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) PdI EE(%)
F1 PRE 10 KELP 10 10 253.7 0.076 49
F10 PRE 10 KRH40 10 10 298.0 0.416 26
F11 PRE 10 T80 10 10 647.1 0.303 58
F12 PRE 10 KELP+T80 10 10 288.5 0.413 61

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) PdI EE(%)
F12 PRE 10 50:50 10 10 288.5 0.413 61
F13 PRE 10 60:40 10 10 266.9 0.596 59
F14 PRE 10 70:30 10 10 256.3 0.563 59
F15 PRE 10 80:20 10 10 241.6 0.283 51

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) PdI EE(%)
F16 PRE 10 0.15 10 10 309.7 1.000 63
F14 PRE 10 0.20 10 10 256.3 0.563 59
F17 PRE 10 0.25 10 10 215.8 0.026 48

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

Media Model
Zero order (R2) First order (R2) Higuchi (R2) Korsemeyer–Peppas
R2 Diffusion exponent (n)
0.1 N HCL 0.487 0.585 0.689 0.986 0.415
PBS pH 6.8 0.866 0.940 0.970 0.984 0.434
PBS pH 7.4 0.870 0.959 0.971 0.985 0.481
Three stage multimedia 0.416 0.640 0.961 0.837 0.264

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) PdI EE(%)
F1 PRE 10 KELP 10 10 253.7 0.076 49
F9 PRE 12.5 KELP 10 10 299.0 0.217 53

Effect of STM on particle size, PDI and EE.

Batch No. SL (0.5%w/v) OLZ (mg) Surfactant (0.2%w/v) 70:30 VD (mL) ST (min) STM Particle size (nm) PdI EE(%)
F20 PRE 10 KELP+T80 10 10 2-8 285.8 0.425 38
F19 PRE 10 KELP+T80 10 10 RT 238.0 0.274 67

Screening of adsorbents.

Adsorbent Mannitol Lactose KCL NUS2 NUS2 + Mannitol NUS2 + Lactose NUS2 + ACL
Particle size (nm) 401.2 308.4 382.9 364.8 361.9 463.3 302.4
PdI 0.400 0.298 0.455 0.410 0.599 0.852 0.494
HR Poor Fair Passable Passable Good Good Good
CI Poor Fair Fair Fair Good Good Good
Angle of repose Excellent Excellent good Excellent Excellent Excellent Excellent
Remarks Fungal growth Particles in the range of 5000 nm also present Rat Holing - Fungal growth Particles 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) PdI EE (%)
F1 PRE 10 KELP 10 10 253.7 0.076 49
F2 GMS 10 KELP 10 10 527.0 0.709 54
F3 CMPR 10 KELP 10 10 630.0 1.000 47
F4 PRE + GMS 10 KELP 10 10 328.2 0.312 50
F5 PRE+CMPR 10 KELP 10 10 164.0 0.482 40
F6 GMS+CMPR 10 KELP 10 10 719.3 0.203 45

Effect of VD on particle size, PDI and EE.

Batch No. SL (0.5%w/v) OLZ (mg) Surfactants (0.2%w/v) 70:30 VD (mL) ST (min) Particle size (nm) PdI EE(%)
F21 PRE 10 KELP+T80 5 10 222.2 0.031 31
F19 PRE 10 KELP+T80 10 10 238.0 0.274 67
eISSN:
2453-6725
Langue:
Anglais
Périodicité:
2 fois par an
Sujets de la revue:
Pharmacy, other
RSS Feed de la revue