RESUMO
AIM: The work reports a novel nanophytosomal gel encapsulating Alpinia galanga (L.) Willd leaf essential oil to treat periodontal infections. METHODS: Alpinia oil-loaded nanophytosomes (ANPs) were formulated by lipid layer hydration technique and were evaluated by FESEM, cryo-TEM, loading efficiency, zeta potential, particle size, release profile etc. Selected ANPs-loaded gel (ANPsG) was evaluated by both in vitro and in vivo methods. RESULTS: Selected ANPs were spherical, unilamellar, 49.32 ± 2.1 nm size, 0.45 PDI, -46.7 ± 0.8 mV zeta potential, 9.8 ± 0.5% (w/w) loading, 86.4 ± 3.02% (w/w) loading efficiency with sustained release profile. ANPsG showed good spreadability (6.8 ± 0.3 gm.cm/sec), extrudability (79.33 ± 1.5%), viscosity (36522 ± 0.82 cps), mucoadhesive strength (44.56 ± 3.5 gf) with sustained ex vivo release tendency. Satisfied ZOI and MIC was observed for ANPsG against periodontal bacteria vs. standard/control. ANPsG efficiently treated infection in ligature induced periodontitis model. Key pharmacokinetic parameters like AUC, MRT, Vd were enhanced for ANPsG. CONCLUSION: ANPsG may be investigated for futuristic clinical studies.
RESUMO
Effective treatment of vaginal infections with conventional antibiotics often faces challenges like unavoidable dose-related side effects with increased risk of bacterial resistance. The study aims to deliver linezolid through natural gum based mucoadhesive nano lipogel to improve therapeutic effectiveness against vaginal infections. The linezolid loaded nanoliposomes (LNLs) were developed by thin film hydration method and were characterized by FTIR, DSC, XRD, FESEM, particle size analysis, zeta potential, drug loading capacity, in vitro release study etc. Selected LNLs was loaded into suitable gel formulation containing Aegle marmelos gum (as the mucoadhesive agent) and evaluated for in vitro, in vivo potentiality. FTIR/DSC test confirmed absence of any major interaction between selected drug and excipients. XRD showed amorphization of the drug encapsulated in NLs. FESEM studies showed spherical LNLs having smooth surface. LNLs had nanosize (51.03 nm), negative surface charge (-25.7 mV), satisfied drug loading capacity (11.5 ± 0.7 %) with sustained drug release. The experimental LNLs loaded lipogel showed desired physico-chemical properties viz. viscosity (37000 cps), spreadability (6.5 gm.cmsec-1), mucoadhesion (21.9 gf) and 61.04 % release of drug across rabbit vaginal mucosal membrane. The nanolipo gel exhibited improved antimicrobial activity against E. coli and C. albicans with respect to the pure linezolid. A good correlation was observed in between in vitro drug release and ex vivo permeation. Improved pharmacokinetic parameters like AUC, AUMC, MRT, Vd was observed for experimental nanolipo gel Vs. marketed formulation. The experimental nanolipo gel could be explored further for futuristic clinical application.
