Ocular administration of acetazolamide microsponges in situ gel formulations

Obiedallah, Manar M.; Abdel-Mageed, A.M.; El-Faham, T. H.

doi:10.1016/j.jsps.2018.01.005

Cited by 66 publications

(42 citation statements)

References 38 publications

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“…This nding supports the explanation of reduced rate of release after increasing the concentration of ethyl cellulose which is matrix former with higher concentration of the polymer increasing the degree of crosslinking and reducing the porosity of the matrix. Similar release pattern was recorded from ethyl cellulose-based particles [36,37].…”

Section: Dsc Studysupporting

confidence: 78%

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Abdalla

Osman

Nouh

et al. 2021

Preprint

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The oral absorption and hence the oral bioavailability of carbamazepine (CBZ) is variable even after administration of rapidly dissolving formulation. This problem was attributed to supersaturation of CBZ and transformation to the less soluble carbamazepine dihydrate (CBD). Accordingly, formulation of sustained release products of CBZ is a promising approach to overcome this problem. Microsponges is an emerging formulation which can help in this direction. The aim of this work was to optimize the composition of microsponges for better encapsulation and sustained release of CBZ for oral administration. CBZ microsponges were prepared using quasi emulsion solvent diffusion technique with varying composition of ethyl cellulose and polyvinyl alcohol (PVA). Microsponges were evaluated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction. Production yield, entrapment efficiency and surface morphology of microsponges were assessed in addition to drug release. Optimum formulation was administered orally to albino rabbits to evaluate the oral bioavailability with reference to unprocessed CBZ. The Instrumental analysis reflected the encapsulation of CBZ in amorphous or molecularly dispersed form in the microsponges. The size and entrapment efficiency of the microsponges increased with increasing polymer contents. This was associated with reduction in CBZ release. Optimum formulation enhanced the oral absorption of CBZ. This was manifested by 2.6-fold increase in the area under the plasma concentration versus time curve compared to that of unprocessed CBZ. The study introduced microsponges as promising carriers for sustained oral delivery of CBZ.

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Section: Dsc Studysupporting

confidence: 78%

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Abdalla

Osman

Nouh

et al. 2021

Preprint

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“…The combined supernatant was then diluted to (10 mL) with pH buffered by acetate (5.8). Using a UV-Vis spectrophotometer (Shimadzu UV 1650 Spectrophotometer, Kyoto, Japan) at λ max 265.8 and 286.4 nm, the concentration of unentrapped ACZ and CAR, respectively, was determined spectrophotometrically compared to the original drug added [ 20 , 21 ].…”

Section: Methodsmentioning

confidence: 99%

“…Carvedilol (CAR) was purchased from Hetero Drugs Company, Telangana, India, and supplied by Multipharma Pharmaceutical Company, Heliopolis, Cairo, Egypt. Polyoxyethylene (20) sorbitan monolaurate (Tween ® 20) was obtained from Nice Chemicals Private Limited Company, Kerala, India. Polyethylene glycol sorbitan monostearate (Tween ® 60) was obtained from Alpha Chemika Company, Mumbai, India.…”

Section: Drugs Chemicals and Reagent Kitsmentioning

confidence: 99%

Formulation and Characterization of Acetazolamide/Carvedilol Niosomal Gel for Glaucoma Treatment: In Vitro, and In Vivo Study

Abdelmonem¹,

Elhabal²,

Abdelmalak³

et al. 2021

Pharmaceutics

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Acetazolamide (ACZ) is a diuretic used in glaucoma treatment; it has many side effects. Carvedilol (CAR) is a non-cardioselective beta-blocker used in the treatment of elevated intraocular pressure; it is subjected to the first-pass metabolism and causes fluids accumulation leading to edema. This study focuses on overcoming previous side effects by using a topical formula of a combination of the two previous drugs. Sixty formulations of niosomes containing Span 20, Span 60, Tween 20, and Tween 60 with two different ratios were prepared and characterized. Formulation with the lowest particle size (416.30 ± 0.23), the highest zeta potential (72.04 ± 0.43 mv), and the highest apparent coefficient of corneal permeability (0.02 ± 0.29 cm/h) were selected. The selected formula was incorporated into the gel using factorial design 23. Niosomes (acetazolamide/carvedilol) consisting of Span 60 and cholesterol in the molar ratio (7:6), HMPC, and carbopol with two different ratios were used. The selected formula was subjected to an in vivo study of intraocular pressure in ocular hypertensive rabbits for 60 h. The sustained gel formula of the combination decreased (IOP) to normal after 1 h and sustained efficacy for 4 days. Histological analysis of rabbit eyeballs treated with the selected formula showed improvement in glaucomatous eye retinal atrophy.

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“…Essential oils with antibacterial activity [114,115] and drugs [116][117][118] have shown interesting results in topical delivery, when loaded into microsponges, over different wound infected models. Other potential topical applications are ocular use [119], and antifungal vaginal formulations [120].…”

Section: Future Perspectives and Conclusionmentioning

confidence: 99%

Ozonated Oils as Antimicrobial Systems in Topical Applications. Their Characterization, Current Applications, and Advances in Improved Delivery Techniques

Ugazio

Tullio²,

Binello

et al. 2020

Molecules

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The search for a wide spectrum of antimicrobial agents that can avoid resistance while maintaining reasonable side effects has led to ozonated oils experiencing an increase in scientific interest and clinical applications. The treatment of vegetable oils with ozone leads to the creation of a reservoir of ozone that slowly releases into the skin thanks to the fact that ozone can be held as ozonides of unsaturated fatty acids. Interest in the use of ozonated oils has meant that several ozonated-vegetable-oil-containing products have been commercialized as cosmetic and pharmaceutical agents, and in innovative textile products with antibacterial activity. New approaches to the delivery of ozonated oils have very recently appeared in an attempt to improve their characteristics and reduce drawbacks, such as an unpleasant odor, high viscosity and undesired effects on skin, including irritation and rashes. The present review focuses on the current status of delivery agents that use ozonated oils as antimicrobial agents in topical (dermal, skin, and soft tissues) treatments. Challenges and future opportunities for these delivery systems will also be discussed.

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Ocular administration of acetazolamide microsponges in situ gel formulations

Cited by 66 publications

References 38 publications

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Microsponges for controlled release and enhanced oral bioavailability of carbamazepine

Formulation and Characterization of Acetazolamide/Carvedilol Niosomal Gel for Glaucoma Treatment: In Vitro, and In Vivo Study

Ozonated Oils as Antimicrobial Systems in Topical Applications. Their Characterization, Current Applications, and Advances in Improved Delivery Techniques

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