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        Formulation, in vitro and in vivo evaluation of lidocaine HCl ocular inserts for topical ocular anesthesia

        Shukr, Marwa 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.7

        Topical anesthesia is a safe and cost-effective method considered as the first-choice in many procedures. The objective of the present study was to develop ocular inserts as a new form of lidocaine HCl to give a sufficient level of anesthetic. Ocuserts were prepared using HPMC and PVA in different ratios with lidocaine HCl alone and lidocaine HCl ${\beta}$-cyclodextrins complex. Drug polymer interactions were studied by Fourier transform infrared spectroscopic studies. The prepared ocular inserts were characterized by means of ocusert thickness, weight variation, folding endurance, surface pH, moisture absorption, drug content and in-vitro drug release. Stability study was conducted on selected formulations, and in vivo evaluation of lidocaine HCl was also carried out. The results revealed that F7 formulations containing drug ${\beta}$-cyclodextrins with 4 % HPMC and 2 % PVA were found to have good physical characteristics and appropriate flexibility. In addition to the highest initial and cumulative percentage of drug released in vitro. The selected F7 ocuserts retained their characteristics during the stability study. The results of in vivo study showed that the addition of ${\beta}$-cyclodextrins in F7 significantly increase the drug content in the aqueous humor when compared with F3 ocuserts containing lidocaine HCl alone.

      • KCI등재

        Formulation, in vitro and in vivo evaluation of lidocaine HCl ocular inserts for topical ocular anesthesia

        Marwa Shukr 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.7

        Topical anesthesia is a safe and cost-effectivemethod considered as the first-choice in many procedures. The objective of the present study was to develop ocularinserts as a new form of lidocaine HCl to give a sufficientlevel of anesthetic. Ocuserts were prepared using HPMCand PVA in different ratios with lidocaine HCl alone andlidocaine HCl b-cyclodextrins complex. Drug polymerinteractions were studied by Fourier transform infraredspectroscopic studies. The prepared ocular inserts werecharacterized by means of ocusert thickness, weight variation,folding endurance, surface pH, moisture absorption,drug content and in-vitro drug release. Stability study wasconducted on selected formulations, and in vivo evaluationof lidocaine HCl was also carried out. The results revealedthat F7 formulations containing drug b-cyclodextrins with4 % HPMC and 2 % PVA were found to have goodphysical characteristics and appropriate flexibility. Inaddition to the highest initial and cumulative percentage ofdrug released in vitro. The selected F7 ocuserts retainedtheir characteristics during the stability study. The resultsof in vivo study showed that the addition of b-cyclodextrinsin F7 significantly increase the drug content in theaqueous humor when compared with F3 ocuserts containinglidocaine HCl alone.

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