Design and Evaluation of a Brinzolamide Drug–Resin &lt;i&gt;in Situ&lt;/i&gt; Thermosensitive Gelling System for Sustained Ophthalmic Drug Delivery

Li, Jing; Hua, Liu; Liu, Li‐Li; Cai, Chao-nan; Xin, Hong-xia; Liu, Wei

doi:10.1248/cpb.c14-00451

Cited by 43 publications

(20 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…T gel of the sol-gels were measured through the magnetic stirring method as described previously ( Li et al, 2014 ). The sol-gels (F1-F8) were diluted with simulated tear fluid (STF) at 6:1 (v/v) ratio.…”

Section: Methodsmentioning

confidence: 99%

Thermoresponsive sol-gel improves ocular bioavailability of Dipivefrin hydrochloride and potentially reduces the elevated intraocular pressure in vivo

Alkholief

Kalam

Almomen

et al. 2020

Saudi Pharmaceutical Journal

View full text Add to dashboard Cite

The present study involves the development of Dipivefrin hydrochloride (DV) containing Poloxamers (P407 and P188)-Carbopol-934 (CP) based thermoresponsive-gels for the management of elevated intraocular pressure (IOP). Optimal formulation was evaluated for gelation temperature (T gel ), physicochemical and viscoelastic properties, in-vitro gel dissolution and drug release studies. The in-vivo safety, precorneal retention, ocular pharmacokinetics and efficacy in reducing IOP were also evaluated. T gel of DV-containing thermoresponsive-gels were between 35.1 and 38.9 °C and it was Poloxamers and CP concentrations dependent. The optimal formulation (F8), composed of 20% P407, 5% P188 and 0.15% CP (w/v), had a T gel of 35 °C. Its viscosity indicated good flow at room temperature and ability to convert to gel at ocular temperature and the rheology studies revealed favorable characteristics for its ocular use. In precorneal retention experiment, F8 indicated significantly higher area under concentrations curves as compared to DV-aqueous suspension (DV-AqS). In-vivo ocular pharmacokinetics indicated a significant improvement in ophthalmic bioavailability of epinephrine (active form of DV). F8 was non-irritant to the eyes and showed a successful, continuous and superior ability to reduce IOP compared to DV-AqS in rabbits. In conclusion, our developed system could be an appropriate substitute to the conventional DV eye preparations in the management of elevated IOP.

show abstract

Section: Methodsmentioning

confidence: 99%

Thermoresponsive sol-gel improves ocular bioavailability of Dipivefrin hydrochloride and potentially reduces the elevated intraocular pressure in vivo

Alkholief

Kalam

Almomen

et al. 2020

Saudi Pharmaceutical Journal

View full text Add to dashboard Cite

show abstract

“…Drugs release slow along with the gel to achieve the purpose of sustained-release. The in vitro process of thermo sensible in situ gel form of many drugs indicated that the release of this drug could sustain 4 ~ 7 days [23,28,29], which highly accorded with the medication cycle (3 ~ 5 days) in veterinary clinical application.…”

mentioning

confidence: 87%

Pharmacokinetic Studies of an In Situ Forming Gel System for Controlled Delivery of Enrofloxacin In Pigs

Yu¹,

Li²,

Zhang³

et al. 2018

SOJPPS

View full text Add to dashboard Cite

or s.c. (subcutaneous) injection [1, 2, 27, 31, 35]Thereby, the recommended dosing regimen of ENR conventional injection was administrated a single 2.5 ~ 5 mg/kg b.w. per day or twice a day, meaning that a course of treatment needs multiple dosing [40]. Obviously, in the clinical application the conventional injection caused a lot of inconvenience, for example, repeated stress response maybe worsen animals' illness or result in more disease, and the drugs' action was not sufficient when it was in peaks and valleys, what's more, frequency administration spent great human, financial and material resources.

show abstract

“…34 Briefly, six healthy New Zealand White rabbits were chosen and divided into BH-solution and Mt-BH-LP groups. Samples (50 µL) were dropped into conjunctival sacs of rabbits, and then the eyes were closed for 1 minute.…”

Section: In Vivo Precorneal Retention Of Mt-bh-lpsmentioning

confidence: 99%

A novel ion-exchange carrier based upon liposome-encapsulated montmorillonite for ophthalmic delivery of betaxolol hydrochloride

Huang¹,

Qi²,

Hou³

et al. 2017

IJN

View full text Add to dashboard Cite

As a novel ion-exchange carrier with high surface area and excellent exchangeability, montmorillonite (Mt) was intercalated with betaxolol hydrochloride (BH) to form a nanocomposite and then encapsulated by liposomes (Mt-BH-LPs) for an ophthalmic drug-delivery system. The Mt-BH and Mt-BH-LPs were prepared by an acidification process and ethanol injection combined with ammonium sulfate gradient methods. The successful formation of Mt-BH and Mt-BH-LPs was verified by thermogravimetric analysis, X-ray diffraction, Fourier-transform infrared spectra, and transmission electron microscopy. Mt-BH-LPs possessed the favorable physical characteristics of encapsulation efficiency, drug loading, mean particle size, and ζ-potential. In vitro release studies indicated Mt-BH-LPs effectively maintained a relatively sustained slow release. Immortalized human corneal epithelial cell cytotoxicity, in vivo rabbit eye-irritation tests, and chorioallantoic membrane–trypan blue staining all revealed that Mt-BH-LPs had no obvious irritation on ocular tissues. A new in vitro tear-turnover model, including inserts containing human corneal epithelial cells, was designed to evaluate the precorneal retention time of Mt-BH-LPs. The results showed that Mt-BH-LPs maintained a certain BH concentration in tear fluid for a longer period than the BH solution. In vivo precorneal retention studies also indicated Mt-BH-LPs prolonged drug retention on the ocular surface more than the BH solution. Furthermore, pharmacodynamic studies showed that Mt-BH-LPs had a prolonged effect on decreasing intraocular optical pressure in rabbits. Our results demonstrated that Mt-BH-LPs have potential as an ophthalmic delivery system.

show abstract

Design and Evaluation of a Brinzolamide Drug–Resin <i>in Situ</i> Thermosensitive Gelling System for Sustained Ophthalmic Drug Delivery

Cited by 43 publications

References 31 publications

Thermoresponsive sol-gel improves ocular bioavailability of Dipivefrin hydrochloride and potentially reduces the elevated intraocular pressure in vivo

Thermoresponsive sol-gel improves ocular bioavailability of Dipivefrin hydrochloride and potentially reduces the elevated intraocular pressure in vivo

Pharmacokinetic Studies of an In Situ Forming Gel System for Controlled Delivery of Enrofloxacin In Pigs

A novel ion-exchange carrier based upon liposome-encapsulated montmorillonite for ophthalmic delivery of betaxolol hydrochloride

Contact Info

Product

Resources

About