Albumin nanoparticles for the delivery of gabapentin: Preparation, characterization and pharmacodynamic studies

• Published in: International journal of pharmaceutics 2014-10, Vol.473 (1-2), p.73-79
• Main Authors: Wilson, Barnabas, Lavanya, Y., Priyadarshini, S.R.B., Ramasamy, Muthu, Jenita, Josephine Leno
• Format: Article
• Language: English
• Subjects: Albumin nanoparticles; Amines - administration & dosage; Amines - chemistry; Amines - pharmacokinetics; Animals; Anticonvulsants - administration & dosage; Anticonvulsants - chemistry; Anticonvulsants - pharmacokinetics; Brain - metabolism; Brain drug targeting; Convulsion; Cyclohexanecarboxylic Acids - administration & dosage; Cyclohexanecarboxylic Acids - chemistry; Cyclohexanecarboxylic Acids - pharmacokinetics; Disease Models, Animal; Drug Carriers - administration & dosage; Drug Carriers - chemistry; Drug Carriers - pharmacokinetics; Drug Compounding; Electroshock; Gabapentin; gamma-Aminobutyric Acid - administration & dosage; gamma-Aminobutyric Acid - chemistry; gamma-Aminobutyric Acid - pharmacokinetics; Male; Nanoparticles - administration & dosage; Nanoparticles - chemistry; Pentylenetetrazole; Polysorbates - administration & dosage; Polysorbates - chemistry; Polysorbates - pharmacokinetics; Rats, Wistar; Seizures - drug therapy; Serum Albumin, Bovine - administration & dosage; Serum Albumin, Bovine - chemistry; Serum Albumin, Bovine - pharmacokinetics
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2014.05.056

[Display omitted] The study was aimed to prepare and evaluate gabapentin loaded albumin nanoparticles and to find out their effectiveness in treating epilepsy. Albumin nanoparticles of gabapentin were prepared by pH-coacervation method. The drug was administered into animals as free drug, gabapentin bound with nanoparticles, and gabapentin bound with nanoparticles coated with polysorbate 80. The polysorbate 80 coated nanoparticles increased the gabapentin concentration in the brain about 3 fold in comparison with the free drug. Moreover, the polysorbate 80 coated nanoparticles significantly reduced the duration of all phases of convulsion in both maximal electroshock induced and pentylenetetrazole induced convulsion models in comparison with free drug and drug bound with nanoparticle formulations, which indicates the ability of polysorbate 80 coated nanoparticles to enhance the gabapentin concentration in the brain.