000 02096nam a22001337a 4500
008 250228b |||||||| |||| 00| 0 eng d
100 _aLayla Albaqshi
245 _aFormulation and Optimization of Aripiprazole-Loaded Nanostructured Lipid Carriers for Nose-to-Brain Delivery
300 _ap579-588
520 _aBackground: Low bioavailability, highly variable blood levels and poor clinical efficacy of Aripiprazole (ARP) are primarily linked to its hydrophobic nature. This investigation focused on the formulation of ARP loaded Nanostructured Lipid Carriers (NLCs) incorporated in thermoreversible in situ intranasal gel for brain delivery. Materials and Methods: The high-speed homogenization method was used to formulate ARP loaded NLCs. A factorial design was utilized to optimize the particle size, entrapment efficiency and drug release of NLCs by selecting Tween 80 as a surfactant and stearic acid and castor oil as solid and liquid lipids, respectively. The ARP loaded NLCs thermoreversible in situ gel was fabricated using Poloxamer 407 as a phase transition agent and carbopol 940 as a mucoadhesive agent. The gel formulation was characterized for various pharmaceutical properties and nasal ciliotoxicity. Results: The optimized NLC (Z7) had nano size (~150 nm), good entrapment efficiency (~93%) and higher drug release (~75% in 12 hr). The formulated thermoreversible in situ gel (Z2 G) showed ideal gelling temperature, gel strength, and pH suitable for nasal use in addition to steady drug release and greater permeation. The toxicity study data revealed that the gel is safe for intranasal application. Conclusion: The prepared thermoreversible in situ gel of ARP loaded NLCs showed excellent potential for intranasal use and can be a feasible alternative to oral therapy in schizophrenia.
654 _aSchizophrenia,
_aAripiprazole,
_a Optimization,
_aPoloxamer,
_aThermoreversible gel,
_aIntranasal.
773 0 _0125266
_9109790
_dBanglore Association of Pharmaceutical Tearchers of India
_tIndian Journal of Pharmaceutical Education and Research
_x0019-5464
942 _cJA
999 _c131246
_d131246