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Diazepam-loaded solid lipid nanoparticles: design and characterization.
AAPS PharmSciTech 2009; 10(1):211-9AP

Abstract

The aim of the present study was to investigate the feasibility of the inclusion of a water-insoluble drug (diazepam, DZ) into solid lipid nanoparticles (SLNs), which offer combined advantages of rapid onset and prolonged release of the drug. This work also describes a new approach to prepare suppositories containing DZ-loaded SLN dispersions, as potential drug carrier for the rectal route. Modified high-shear homogenization and ultrasound techniques were employed to prepare SLNs. The effect of incorporation of different concentrations of Compritol ATO 888 or Imwitor 900K and Poloxamer 188 or Tween 80 was investigated. Results showed that varying the type or concentration of lipid matrix or surfactant had a noticeable influence on the entrapment efficiencies, particle size, and release profiles of prepared SLNs. Differential scanning calorimetry and X-ray diffraction measurements showed that the majority of SLNs possessed less ordered arrangements of crystals than the corresponding bulk lipids, which was favorable for increasing the drug loading capacity. Transmission electron microscopy and laser diffractometry studies revealed that the prepared nanoparticles were round and homogeneous and 60% of the formulations were less than 500 nm. Additionally, SLN formulations showed significant (P < 0.05) prolonged release than DZ solution. The subsequent step encompassed the preparation and evaluation of SLN-based suppositories utilizing SLN formulations that illustrated optimal release profiles. The in vitro release of DZ from the suppositories prepared using DZ-loaded SLN dispersions (equivalent to 2 mg DZ) was significantly (P < 0.05) extended compared to suppositories containing 2 mg DZ free drug.

Authors+Show Affiliations

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, Egypt. gabdelbary@gmail.comNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19277870

Citation

Abdelbary, Ghada, and Rania H. Fahmy. "Diazepam-loaded Solid Lipid Nanoparticles: Design and Characterization." AAPS PharmSciTech, vol. 10, no. 1, 2009, pp. 211-9.
Abdelbary G, Fahmy RH. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech. 2009;10(1):211-9.
Abdelbary, G., & Fahmy, R. H. (2009). Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech, 10(1), pp. 211-9. doi:10.1208/s12249-009-9197-2.
Abdelbary G, Fahmy RH. Diazepam-loaded Solid Lipid Nanoparticles: Design and Characterization. AAPS PharmSciTech. 2009;10(1):211-9. PubMed PMID: 19277870.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Diazepam-loaded solid lipid nanoparticles: design and characterization. AU - Abdelbary,Ghada, AU - Fahmy,Rania H, Y1 - 2009/03/10/ PY - 2008/07/14/received PY - 2009/01/31/accepted PY - 2009/3/12/entrez PY - 2009/3/12/pubmed PY - 2009/6/24/medline SP - 211 EP - 9 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 10 IS - 1 N2 - The aim of the present study was to investigate the feasibility of the inclusion of a water-insoluble drug (diazepam, DZ) into solid lipid nanoparticles (SLNs), which offer combined advantages of rapid onset and prolonged release of the drug. This work also describes a new approach to prepare suppositories containing DZ-loaded SLN dispersions, as potential drug carrier for the rectal route. Modified high-shear homogenization and ultrasound techniques were employed to prepare SLNs. The effect of incorporation of different concentrations of Compritol ATO 888 or Imwitor 900K and Poloxamer 188 or Tween 80 was investigated. Results showed that varying the type or concentration of lipid matrix or surfactant had a noticeable influence on the entrapment efficiencies, particle size, and release profiles of prepared SLNs. Differential scanning calorimetry and X-ray diffraction measurements showed that the majority of SLNs possessed less ordered arrangements of crystals than the corresponding bulk lipids, which was favorable for increasing the drug loading capacity. Transmission electron microscopy and laser diffractometry studies revealed that the prepared nanoparticles were round and homogeneous and 60% of the formulations were less than 500 nm. Additionally, SLN formulations showed significant (P < 0.05) prolonged release than DZ solution. The subsequent step encompassed the preparation and evaluation of SLN-based suppositories utilizing SLN formulations that illustrated optimal release profiles. The in vitro release of DZ from the suppositories prepared using DZ-loaded SLN dispersions (equivalent to 2 mg DZ) was significantly (P < 0.05) extended compared to suppositories containing 2 mg DZ free drug. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/19277870/Diazepam_loaded_solid_lipid_nanoparticles:_design_and_characterization_ L2 - https://dx.doi.org/10.1208/s12249-009-9197-2 DB - PRIME DP - Unbound Medicine ER -