Design and evaluation of novel fast forming pilocarpine-loaded ocular hydrogels for sustained pharmacological response

Anumolu, SivaNaga S.; Singh, Yashveer; Gao, Dayuan; Stein, Stanley J.; Sinko, Patrick J.

doi:10.1016/j.jconrel.2009.03.016

Cited by 84 publications

(71 citation statements)

References 42 publications

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“…Simulated Tears 2 (Table 14) in the volume of 4 mL was used to evaluate drug-loading efficiency and in vitro release of pilocarpine from hydrogels. These hydrogels behave as a drug-depot for controlled-release applications (48).The same simulated medium was also used to evaluate the in vitro release of pilocarpine from nanoparticles composed of chitosan and polyacrylic acid (49). Pandit et al (45) developed in situ forming sodium alginate gels for the extended release of indomethacin to the eye.…”

Section: Ophthalmic Routementioning

confidence: 99%

Simulated Biological Fluids with Possible Application in Dissolution Testing

Marques¹,

Löebenberg²,

Almukainzi³

2011

Dissolution Technol.

864

523

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This literature review is a compilation of the composition and, in most cases, the preparation instructions for simulated biological fluids that may be used as dissolution media in the evaluation of dissolution profiles and amount of drug released from pharmaceutical dosage forms. The use of simulated biological fluids can give a better understanding of the release mechanisms and possible in vivo behavior of a product and enhance the predictive capability of the dissolution testing. A summary of the major characteristics of the most used routes of administration that may affect dissolution and absorption of drug substances is presented. The routes and simulated biological fluids covered by this review are:• Parenteral: simulated body fluid and simulated synovial fluid.• Oral: fasted-state simulated gastric fluid, fed-state simulated gastric fluid, fasted-state simulated intestinal fluid, fed-state simulated intestinal fluid, simulated colonic fluid, fasted-state simulated colonic fluid, and fed-state simulated colonic fluid.• Buccal and sublingual: simulated saliva.• Pulmonary: simulated lung fluid.• Vaginal: simulated vaginal fluid and simulated semen.• Ophthalmic: simulated tears.Simulated sweat is also included. Some examples of how these simulated biological fluids are used to evaluate dosage forms are included in each route of administration.

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Section: Ophthalmic Routementioning

confidence: 99%

Simulated Biological Fluids with Possible Application in Dissolution Testing

Marques¹,

Löebenberg²,

Almukainzi³

2011

Dissolution Technol.

864

523

View full text Add to dashboard Cite

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“…The ΔIOP vs. time curve was plotted to compare the efficacy of prepared formulations with the conventional ophthalmic drops and the comparison was done in terms of (1) I max , peak decrease in IOP; (2) t max , time to reach peak IOP decrease; (3) area under the curve (AUC) (ΔIOP vs.t) , area under the ΔIOP vs. time curve; (4) duration of IOP decrease and (5) slope of terminal linear portion of the decrease in IOP vs. time curve (37). The AUC (ΔIOP vs.t) of ΔIOP vs. time curve was calculated using trapezoid rule (also calculated using Graph Pad Prism 4 software).…”

Section: Induction Of Glaucomamentioning

confidence: 99%

Brimonidine Tartrate–Eudragit Long-Acting Nanoparticles: Formulation, Optimization, In Vitro and In Vivo Evaluation

Bhagav

Upadhyay

Chandran³

2011

AAPS PharmSciTech

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Abstract. In the present study, an effort was made to design prolonged release Eudragit nanoparticles of brimonidine tartrate by double emulsion-solvent evaporation technique for the treatment of open-angle glaucoma. The effect of various formulation variables like initial drug amount, lecithin proportion, phase volume and pH, secondary emulsifier and polymer proportion were studied. Various process variables like energy and duration of emulsification, lyophilization on the characteristics of nanoparticles and in vitro drug release profile were studied. The selected formulations were subjected to in vivo intraocular pressure-lowering efficacy studies by administering aqueous dispersion of nanoparticles into the lower cul de sac of glaucomatous rabbits. The prepared Eudragit-based nanoparticles were found to have narrow particle size range and improved drug loading. The investigated process and formulation variables found to have significant effect on the particle size, drug loading and entrapment efficiency, and in vitro drug release profile of nanoparticles. The selected formulations upon in vivo ocular irritability and tolerability tests were found to be well tolerated with no signs of irritation. In vivo pharmacodynamic efficacy studies revealed that the selected nanoparticle formulations significantly improved the therapy as area under the ΔIOP vs. time curve [AUC (ΔIOP vs.t) ] showed several fold increase in intensity and duration of intraocular pressure (IOP) decrease. All the selected nanoparticle formulations were found to prolong the drug release in vitro and prolong IOP reduction efficacy in vivo, thus rendering them as a potential carrier in developing improved drug delivery systems for the treatment of glaucoma.

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“…A value between 0.45 and 0.89 for n is indicative of anomalous transport in which Fickian transport and matrix relaxation occur simultaneously. A value of 0.89 for n indicates case-II relaxational mechanism associated with the stresses and state transitions that occur in the swelling (24)(25)(26)(27)(28)(29).…”

Section: Evaluation Of the Release Mechanismmentioning

confidence: 99%

Design and In Vitro Evaluation of Capsaicin Transdermal Controlled Release Cubic Phase Gels

et al. 2010

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Abstract. The purpose of this study was to design and investigate the transdermal controlled release cubic phase gels containing capsaicin using glycerol monooleate (MO), propylene glycol (1,2-propanediol, PG), and water. Three types of cubic phase gels were designed based on the ternary phase diagram of the MO-PG-water system, and their internal structures were confirmed by polarizing light microscopy (PLM) and small-angle X-ray scattering (SAXS). Release results showed the cubic phase gels could provide a sustained system for capsaicin, while the initial water content in the gels was the major factor affecting the release rate. Release kinetics was determined to fit Higuchi's square-root equation indicating that the release was under diffusion control. The calculated diffusion exponent showed the release from cubic phase gels was anomalous transport. The unique structure of the cubic phases, capsaicin distributed in the lipid bilayers, and cubic phase gel swelling contributed to the release mechanism. The cubic phase gel may be an interesting application for transdermal delivery system of capsaicin in alleviating the post-incision pain.

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Design and evaluation of novel fast forming pilocarpine-loaded ocular hydrogels for sustained pharmacological response

Cited by 84 publications

References 42 publications

Simulated Biological Fluids with Possible Application in Dissolution Testing

Simulated Biological Fluids with Possible Application in Dissolution Testing

Brimonidine Tartrate–Eudragit Long-Acting Nanoparticles: Formulation, Optimization, In Vitro and In Vivo Evaluation

Design and In Vitro Evaluation of Capsaicin Transdermal Controlled Release Cubic Phase Gels

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