Study of the extent of ocular absorption of acetazolamide from a developed niosomal formulation, by microdialysis sampling of aqueous humor

Aggarwal, Deepika; Pal, Dhananjay; Mitra, Ashim K.; Kaur, Indu Pal

doi:10.1016/j.ijpharm.2007.01.019

Cited by 79 publications

(33 citation statements)

References 20 publications

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“…This effect might be due to the improvement in the concentration of hydrophilic drugs in the inner water phase by the reversephase evaporation method, leading to the formation of large unilamellar vesicles. 35,36 In the uniform design, the EE was improved by increasing the phospholipid concentration in experimental formulations. Similar findings were previously reported by Shen et al and Fang et al 17,37 Glycerosomes are a kind of closed vesicles with a lipid bilayer structure similar to the biomembrane.…”

Section: Discussionmentioning

confidence: 99%

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Zhang

et al. 2017

IJN

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In this study, a novel glycerosome carrier containing essential oils was prepared for topical administration of paeoniflorin (PF) to enhance its transdermal drug delivery and improve drug absorption in the synovium. The formulation of glycerosomes was optimized by a uniform design, and the final vehicle was composed of 5% (w/v) phospholipid, 0.6% (w/v) cholesterol, and 10% (v/v) glycerol, with 2% (v/v) Speranskia tuberculata essential oil (STO) as the transdermal enhancer. The in vitro transdermal flux of PF loaded in the STO-glycerosomes was 1.4-fold, 1.6-fold, and 1.7-fold higher than those of glycerosomes, liposomes, and tinctures, respectively. In vivo studies showed that the use of STO-glycerosomes was associated with a 3.1-fold greater accumulation of PF in the synovium than that of common glycerosomes. This finding was confirmed by in vivo imaging studies, which found that the fluorescence intensity of Cy5.5-loaded STO-glycerosomes in mice knee joints was 1.8-fold higher than that of the common glycerosomes 5 h after administration. The glycerosomes mediated by STO exhibited considerable skin permeability as well as improved drug absorption in the synovium, indicating that STO-glycerosomes may be a potential PF transdermal delivery vehicle for the treatment of rheumatoid arthritis caused by synovium lesions.

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Section: Discussionmentioning

confidence: 99%

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Zhang

et al. 2017

IJN

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“…76) In this study, no change in IOP was observed in the untreated eye during the course of measurement in any of the formulations, thus indicating that these formulations exerted a local action within the eye and that the observed IOP lowering activity is not because of any systemic absorption. [77][78][79] After instillation of ATS, the T max was reached after 1.00 h of instillation, followed by a rapid decline of the percentage decrease in IOP indicating its short duration of action. In case of ATG, T max was observed at 2.00 h, but the effect was not sustained sufficiently and diminished after 6 h. ATN showed a significant effect which was sustained for up to 7 h. On the other hand, ATNG showed promising results as it significantly decreased the IOP to maximum value (49.80%) after 4.33 h of drug administration, and the effect was sustained and prolonged for the time of the experiment up till 8 h. The AUC after application of atenolol formulations until 8 h were 2.22, 2.85, 4.58-fold higher than that of atenolol solution for ATG, ATN, and ATNG, respectively.…”

Section: )mentioning

confidence: 99%

“…58,44) Carbopols is an important class of ocular bioadhesives. 79) Due to the low viscosity of colloidal suspensions of vesicles that does not allow sufficient retention time of the dosage form in the eye upon instillation, different hydrogel matrices such as carbopol have been used to increase the viscosity of topical preparation and to increase the retention time of the formulation at the site of administration due to good bioadhesive properties. 83) Our results have shown that 0.5% (w/v) atenolol niosomal hydrogel extended the duration of action for 8 h with 4.33 fold increase in the AUC than that of 0.5% (w/v) atenolol solution.…”

Section: )mentioning

confidence: 99%

Potential Use of Niosomal Hydrogel as an Ocular Delivery System for Atenolol

Hashim

El-Dahan

Yusif

et al. 2014

Biological & Pharmaceutical Bulletin

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Niosomes have been reported as possible approach to improve the low corneal penetration and bioavailability characteristics for many drugs. The purpose of this study was to prepare and characterize an effective ocular niosomal hydrogel containing 0.5% (w/v) atenolol which is β1 adrenoceptor blocker for treatment of glaucoma. Thin film hydration method was used for the preparation of niosomes using Span 60 and cholesterol at different molar ratios. Niosomes were characterized using laser diffraction particle size analyzer, transmission electron microscopy, and differential scanning calorimetry. The results showed that higher entrapment efficiency (80.7% 1.2) was obtained from niosomes prepared using Span 60/cholesterol at a 2 : 1 molar ratio. Stability study revealed that a fairly high retention of atenolol inside vesicles (83.1% 2.35) up to a period of 3 months at 4°C. It was found that niosomal hydrogel formulation using carbopol 934P significantly exhibited sustained in vitro release of the drug compared with free drug solution and other polymeric hydrogels. The intraocular pressure (IOP) lowering activity of selected atenolol formulations was determined and compared with that of atenolol solution. It is worth noting that niosomal hydrogel formulation was found to show the most significant prolonged decrease in IOP, suggesting that niosomal hydrogel could be a promising delivery system for atenolol.

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“…Topical delivery is not much successful because of its low solubility in tear fluid (1.9 mg/ml) and low permeability profile. Many researchers have tried many formulations to increase topical ocular bioavailability of ACZ like liposomes, niosomes, cyclodextrin complex, etc (Kaur et al, 2000(Kaur et al, , 2002Aggarwal et al, 2007;Granero, 2008;Palma et al, 2009). Nanoparticles' (NPs) unique size and other properties make it suitable for ocular delivery.…”

Section: Introductionmentioning

confidence: 99%

Development,in vitroandin vivocharacterization of Eudragit RL 100 nanoparticles for improved ocular bioavailability of acetazolamide

Verma

Gupta

Jha³

et al. 2013

Drug Delivery

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Glaucoma is characterized by increased intra ocular pressure (IOP) which results in blindness if left untreated. Acetazolamide (ACZ) is used to treat glaucoma since long back. Since it is a Class IV drug [According to Biopharmaceutics Classification System (BCS)], so its topical delivery results in poor ocular bioavailability. Objective of the present study is to increase the topical ocular bioavailability and to sustain the release of drug for longer time. ACZ-loaded Eudragit Õ RL 100 nanoparticle suspension (ACZ-E-NPs) was prepared by the nanoprecipitation method. Ratio of organic to aqueous phase and composition of organic phase were altered to get the best formulation. Formulations prepared with acetone and methanol as organic phase were smallest in size. EE was in the range of 57.8% to 68.5%. According to drug release study almost all the formulations released 80% of drug in 8 h duration. The kinetics of drug release showed that the drug release pattern followed Higuchi's model (highest R 2 values) and further it was fitted to the Korsemeyer-Peppas model, which showed the release was as per Fickian diffusion. IOP lowering effects of plain drug solution and ACZ-E-NPs were compared in adult male albino rabbits with a Riester Tonometer. The data revealed that the ACZ-E-NPs lower the IOP for longer time and of higher magnitude also. The difference was significant (p50.001). Short-term stability study showed that none of the formulations was having remarked difference in their physicochemical properties after 6 months of storage at various temperatures.

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Study of the extent of ocular absorption of acetazolamide from a developed niosomal formulation, by microdialysis sampling of aqueous humor

Cited by 79 publications

References 20 publications

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Essential oil-mediated glycerosomes increase transdermal paeoniflorin delivery: optimization, characterization, and evaluation in vitro and in vivo

Potential Use of Niosomal Hydrogel as an Ocular Delivery System for Atenolol

Development,in vitroandin vivocharacterization of Eudragit RL 100 nanoparticles for improved ocular bioavailability of acetazolamide

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