Thermo-sensitive gel in glaucoma therapy for enhanced bioavailability: In vitro characterization, in vivo pharmacokinetics and pharmacodynamics study

Zeng, Youmei; Chen, Jintian; Li, Yanrong; Huang, Jiayuan; Huang, Zhengwei; Huang, Ying; Pan, Xin; Wu, Chuanbin

doi:10.1016/j.lfs.2018.09.050

Cited by 35 publications

(25 citation statements)

References 34 publications

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“…Glaucoma symptoms include blurred vision, headache, hallows in vision, and progressive loss of vision. It is the most serious ocular disease requiring a lifetime treatment to prevent symptoms and progression of the disease (Mishra & Jain, 2014; Zeng et al., 2018). Pharmacological treatment of glaucoma based on either decreasing production of aqueous humor or increasing its drainage to restore the balance and prevent the buildup of aqueous humor.…”

Section: Introductionmentioning

confidence: 99%

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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Brimonidine tartrate (BRT) is a hydrophilic a 2 adrenergic agonist used for the treatment of glaucoma. Glaucoma is an ocular disease affecting the anterior segment of the eye requiring lifetime treatment. Owing to the obstacles facing ocular delivery systems and hydrophilicity of BRT, frequent administration of the eye drops is required. Niosomes have been widely used to improve the ocular bioavailability of the topically applied drugs and to enhance the ocular residence time. However, they have drawbacks as physical instability, aggregation, and loss of the entrapped drug. For this reason, BRT proniosomes were prepared to overcome niosomal instability issues. A D-optimal design was utilized to determine the optimum conditions for preparation of the proniosomal gels. Independent variables were amount of surfactant, surfactant:cholesterol ratio, and type of surfactant used. The dependent variables were entrapment efficiency (EE%), particle size, percentage of drug released after 2 h (Q 2h), and percentage of drug released after 24 h (Q 24h). The optimum formula was suggested with desirability 0.732 and the composition of 540 mg Span 60 and 10:1 surfactant:cholesterol ratio. The results obtained after reconstitution were; EE% of 79.23 ± 1.12% particle size of 810.95 ± 16.758 nm, polydispersity index (PDI) 0.6785 ± 0.213, zeta potential 59.1 ± 0.99 mV, Q 2h 40.98 ± 1.29%, Q 8h 63.35 ± 6.07%, and Q 24h ¼ 91.11 ± 1.76%. Transmission electron microscope imaging of the formula showed the typical spherical shape of niosomes. In-vivo pharmacodynamic study assured the improved ocular bioavailability of BRT selected formula when compared with Alphagan V R P with relative AUC 0-24 of 5.024 and 7.90 folds increase in the mean residence time (MRT). Lack of ocular irritation of the formula was assured by Draize test.

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Section: Introductionmentioning

confidence: 99%

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

2019

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“…In an in vivo rabbit model, poloxamer-based in situ gels showed a significantly higher absorption to the aqueous humor of loteprednol [19], methazolamide [20] and timolol [21], compared to standard formulations. However, it has been shown that the delivery of methazolamide and timolol, both anti-glaucoma drugs, did not significantly reduce the intraocular pressure (IOP)…”

Section: J O U R N a L P R E -P R O O Fmentioning

confidence: 92%

“…compared with standard formulations [20,21]. Besides its excellent biocompatibility, poloxamers® exhibited low mechanical strength and rapid erosion.…”

Section: J O U R N a L P R E -P R O O Fmentioning

confidence: 99%

Advances and limitations of drug delivery systems formulated as eye drops

Jumelle

Gholizadeh

Annabi

et al. 2020

Journal of Controlled Release

240

125

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This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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“…The pH value of TSG pre-gel solution was measured by a pH meter (PB-10, Sartorius, Germany) at room temperature. The gelation temperature was measured by a tube inversion method as described by Zeng et al (2018). Briefly, a tube with TSG pre-gel solution inside was heated in water bath at a rate of 1 C/min.…”

Section: Preparation and Characterization Of Tsg And Cip-ms-g-tsgmentioning

confidence: 99%

PLGA microsphere-based composite hydrogel for dual delivery of ciprofloxacin and ginsenoside Rh2 to treat Staphylococcus aureus -induced skin infections

et al. 2020

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When antibiotic-resistant pathogenic bacteria pose a high threat to human health, bacterial multidrug efflux pumps become major contributors to the high-level antibiotic resistance in most microorganisms. Since traditional antibiotics are still indispensable currently, we report a dual drug delivery system to maximize the antibacterial efficacy of antibiotics by inhibiting efflux pumps in bacteria before their exposure to antibiotics. In this research, a microsphere/hydrogel composite was constructed from ciprofloxacin (Cip)-loaded poly (lactic-co-glycolic acid) (PLGA) microspheres and ginsenoside Rh2 (G-Rh2) dispersed thermo-sensitive hydrogel to treat skin infections. In vitro drug release studies indicated that while G-Rh2 in hydrogel presented a faster and short-term release manner to rapidly inhibit the NorA efflux pumps, Cip showed a sustained and long-term release behavior to provide a local high concentration gradient for facilitating drug percutaneous penetration. The combination of Cip and G-Rh2 demonstrated a high degree of synergism against both methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus (MRSA), hence significantly improving their in vitro antibacterial activity and efficiency. Moreover, the antibacterial performance of the microsphere/hydrogel composite with a sequential release profile is superior to that of other formulations in mouse model of MRSA skin infections, indicating its great potential to treat antibiotic-resistant skin infections.

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Thermo-sensitive gel in glaucoma therapy for enhanced bioavailability: In vitro characterization, in vivo pharmacokinetics and pharmacodynamics study

Cited by 35 publications

References 34 publications

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study

Advances and limitations of drug delivery systems formulated as eye drops

PLGA microsphere-based composite hydrogel for dual delivery of ciprofloxacin and ginsenoside Rh2 to treat Staphylococcus aureus -induced skin infections

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