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Investigations of the effect of the lipid matrix on drug entrapment, in vitro release, and physical stability of olanzapine-loaded solid lipid nanoparticles.
AAPS PharmSciTech. 2007 Oct 12; 8(4):E83.AP

Abstract

The purpose of this research was to study the effect of the lipid matrix on the entrapment of olanzapine (OL). OL-loaded solid lipid nanoparticles (SLNs) were prepared using lipids like glyceryl monostearate (GMS), Precirol ATO 5 (PRE), glyceryl tristearate (GTS), and Witepsol E85 (WE 85)--and poloxamer 407 and hydrogenated soya phosphatidylcholine as stabilizers--using a hot melt emulsification high-pressure homogenization technique, and then characterized by particle size analysis, zeta potential, differential scanning calorimetry (DSC), and powder X-ray diffraction (pXRD). Homogenization at 10,000 psi for 3 cycles resulted in the formation of SLNs with a mean particle size of approximately 190 nm for the 4 lipids investigated. The highest partition coefficient for OL between the melted lipid and pH 7.4 phosphate buffer (pH 7.4 PB) was obtained with GTS. The entrapment efficiency was in the following order: GTS SLNs > PRE SLNs > WE 85 SLNs > GMS SLNs. DSC and pXRD showed that much of the incorporated fraction of OL existed in the amorphous state after incorporation into SLNs. A sharp increase in the flocculation of the SLN dispersions was observed upon addition of 0.6 M aqueous sodium sulfate solution. Nanoparticle surface hydrophobicity was in the following order: GTS SLNs > PRE SLNs > WE 85 SLNs > GMS SLNs. A significant increase in size and zeta potential was observed for GTS SLN and WE 85 SLN dispersions stored at 40 degrees C. Release of OL from the SLNs was sustained up to 48 hours in pH 7.4 PB and obeyed Higuchi's release kinetics.

Authors+Show Affiliations

Drug Delivery Research Laboratory, Center of Relevance and Excellence in NDDS, Pharmacy Department, GH Patel Building, Donor's Plaza, Fatehgunj, M.S. University, Baroda - 390002, Gujarat, India.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18181544

Citation

Vivek, K, et al. "Investigations of the Effect of the Lipid Matrix On Drug Entrapment, in Vitro Release, and Physical Stability of Olanzapine-loaded Solid Lipid Nanoparticles." AAPS PharmSciTech, vol. 8, no. 4, 2007, pp. E83.
Vivek K, Reddy H, Murthy RS. Investigations of the effect of the lipid matrix on drug entrapment, in vitro release, and physical stability of olanzapine-loaded solid lipid nanoparticles. AAPS PharmSciTech. 2007;8(4):E83.
Vivek, K., Reddy, H., & Murthy, R. S. (2007). Investigations of the effect of the lipid matrix on drug entrapment, in vitro release, and physical stability of olanzapine-loaded solid lipid nanoparticles. AAPS PharmSciTech, 8(4), E83. https://doi.org/10.1208/pt0804083
Vivek K, Reddy H, Murthy RS. Investigations of the Effect of the Lipid Matrix On Drug Entrapment, in Vitro Release, and Physical Stability of Olanzapine-loaded Solid Lipid Nanoparticles. AAPS PharmSciTech. 2007 Oct 12;8(4):E83. PubMed PMID: 18181544.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Investigations of the effect of the lipid matrix on drug entrapment, in vitro release, and physical stability of olanzapine-loaded solid lipid nanoparticles. AU - Vivek,K, AU - Reddy,Harivardhan, AU - Murthy,Ramachandra S R, Y1 - 2007/10/12/ PY - 2008/1/10/pubmed PY - 2008/1/25/medline PY - 2008/1/10/entrez SP - E83 EP - E83 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 8 IS - 4 N2 - The purpose of this research was to study the effect of the lipid matrix on the entrapment of olanzapine (OL). OL-loaded solid lipid nanoparticles (SLNs) were prepared using lipids like glyceryl monostearate (GMS), Precirol ATO 5 (PRE), glyceryl tristearate (GTS), and Witepsol E85 (WE 85)--and poloxamer 407 and hydrogenated soya phosphatidylcholine as stabilizers--using a hot melt emulsification high-pressure homogenization technique, and then characterized by particle size analysis, zeta potential, differential scanning calorimetry (DSC), and powder X-ray diffraction (pXRD). Homogenization at 10,000 psi for 3 cycles resulted in the formation of SLNs with a mean particle size of approximately 190 nm for the 4 lipids investigated. The highest partition coefficient for OL between the melted lipid and pH 7.4 phosphate buffer (pH 7.4 PB) was obtained with GTS. The entrapment efficiency was in the following order: GTS SLNs > PRE SLNs > WE 85 SLNs > GMS SLNs. DSC and pXRD showed that much of the incorporated fraction of OL existed in the amorphous state after incorporation into SLNs. A sharp increase in the flocculation of the SLN dispersions was observed upon addition of 0.6 M aqueous sodium sulfate solution. Nanoparticle surface hydrophobicity was in the following order: GTS SLNs > PRE SLNs > WE 85 SLNs > GMS SLNs. A significant increase in size and zeta potential was observed for GTS SLN and WE 85 SLN dispersions stored at 40 degrees C. Release of OL from the SLNs was sustained up to 48 hours in pH 7.4 PB and obeyed Higuchi's release kinetics. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/18181544/Investigations_of_the_effect_of_the_lipid_matrix_on_drug_entrapment_in_vitro_release_and_physical_stability_of_olanzapine_loaded_solid_lipid_nanoparticles_ L2 - https://www.lens.org/lens/search?q=citation_id:18181544 DB - PRIME DP - Unbound Medicine ER -