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

Rajashree Hirlekar; Alfiha Momin; Srinivas Bhairy

doi:10.2478/afpuc-2024-0004

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

European Pharmaceutical Journal

Volume 71 (2024): Issue 1 (August 2024)

By: Rajashree Hirlekar, Alfiha Momin and Srinivas Bhairy

Open Access

|Apr 2024

Figures & Tables

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

Percentage desorption of SLNs from DANs prepared with different adsorbents [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)].

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.

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

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

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
	Zero order (R²)	First order (R²)	Higuchi (R²)	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

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DOI: https://doi.org/10.2478/afpuc-2024-0004 | Journal eISSN: 2453-6725

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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

Keywords:

Olanzapine,

Hepatic metabolism,

Solid lipid nanoparticles,

Dry adsorbed nanoparticles,

Related subjects:

© 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.

Volume 71 (2024): Issue 1 (August 2024)

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

Figures & Tables

Figure 1.

Figure 2.

Figure 3.

Figure 4.

Figure 5.

Figure 6.

Figure 7.

Effect of ST on particle size, PDI and EE_

Effect of LC on particle size, PDI and EE_

Effect of surfactant on particle size, PDI and EE_

Effect of surfactant ratio on particle size, PDI and EE_

Effect of SC on particle size, PDI and EE_

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

Effect of DC on particle size, PDI and EE_

Effect of STM on particle size, PDI and EE_

Screening of adsorbents_

Effect of SL on particle size, PDI and EE_

Effect of VD on particle size, PDI and EE_

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