Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

Attia, I.A.; El‐Gizawy, Sanaa A.; Fouda, Mohammed; Donia, Ahmed M.

doi:10.1208/pt0804106

Cited by 109 publications

(70 citation statements)

References 13 publications

(13 reference statements)

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“…The chains present on both sides of sugar moiety of BRD-BG cause high lipophilicity of the surfactant, hence solubilization of hydrophobic drugs is enhanced (Waddad et al, 2013). The cholesterol content (0.33%) in the lipid phase of the delivery system could also be responsible for increasing the EE of Levofloxacin, as reported by other investigators (Attia et al, 2007).…”

Section: Drug Entrapment Efficiency (Ee)mentioning

confidence: 60%

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

et al. 2016

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Context: Vesicular systems have attracted great attention in drug delivery because of their amphiphilicity, biodegradability, non-toxicity and potential for increasing drug bioavailability. Objective: A novel sugar-based double-tailed surfactant containing renewable block was synthesized for preparing niosomal vesicles that could be exploited for Levofloxacin encapsulation, aiming to increase its oral bioavailability. Materials and methods: The surfactant was characterized by 1 H NMR, mass spectroscopy and Fourier transform infrared spectroscopy (FT-IR). Its biocompatibility was studied against cell cultures and human blood hemolysis. In vivo acute toxicity was evaluated in mice. The vesicle morphology, size, drug-excipients interaction and entrapment efficiency (EE) were examined using atomic force microscope (AFM), dynamic light scattering (DLS), FT-IR and HPLC. Oral bioavailability studies of Levofloxacin in surfactant-based niosomal formulation were carried out using rabbits and plasma samples were analyzed using HPLC. Results and discussion: Vesicles were spherical in shape and the size was 190.31 ± 4.51 nm with a polydispersity index (PDI) of 0.29 ± 0.03. The drug EE in niosomes was 68.28 ± 3.45%. When applied on cell lines, high cell viability was observed even after prolonged exposure at high concentrations. It caused 5.77 ± 1.34% hemolysis at 1000 mg/mL and was found to be safe up to 2000 mg/kg. Elevated Levofloxacin plasma concentration was achieved when delivered with novel vesicles. Conclusion:The surfactant was demonstrated to be safe and effective as carrier of Levofloxacin. The study suggests that this sugar-based double-tailed nonionic surfactant could be promising nano-vesicular system for delivery and enhancing oral bioavailability of the hydrophobic Levofloxacin.

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Section: Drug Entrapment Efficiency (Ee)mentioning

confidence: 60%

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

et al. 2016

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“…Sonication may be responsible for the breakdown of the multilamellar vesicles to form much smaller unilamellar vesicles which is very essential in avoiding the irritation to the eye. 53,54) Nanoparticles less than 200 nm are considered accepted for passive drug targeting and for in vivo study. 55,56) Vesicle size is an important parameter that influences the biopharmaceutical feature of the carrier.…”

Section: Vesicles Preparation and Characterizationmentioning

confidence: 99%

“…These results pointed to sustained release characteristics with a Higuchi pattern of drug release, where niosomes act as a reservoir system for continuous delivery of the drug. 53) CH reduces the leakage or permeability of encapsulating drug by decreasing the niosomal membrane fluidity.…”

Section: )mentioning

confidence: 99%

“…61,65,66) These results pointed to sustained release characteristics with a Higuchi pattern of drug release, where niosomes act as a reservoir system for continuous delivery of the drug. 53) In this study, the Korsmeyer-Peppas equation was utilized to interpret the atenolol release kinetics. It can give more insights on other drug release mechanisms such as Fickian (diffusion), non-Fickian (anomalous), and erosion-mediated (zero-order) release.…”

Section: )mentioning

confidence: 99%

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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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“…So, Attia et al developed ACV niosomes composed by cholesterol, Span 60, and dicetyl phosphate to improve its oral bioavailability with positive results in rabbits. 25) Some strategies to improve the absorption of different drugs from the gastrointestinal tract are based on the use of mucoadhesive delivery systems. Mucoadhesion is a complex phenomenon.…”

mentioning

confidence: 99%

Mucoadhesive Tablets for Controlled Release of Acyclovir

Ruíz-Caro

Gago-Guillan²,

Otero-Espinar³

et al. 2012

CHEMICAL & PHARMACEUTICAL BULLETIN

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Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the tablets behaviour in both fed and fasted states. All the designed tablets showed good mucoadhesive properties on gastric mucosa due to the presence of CS and/or HPMC. In vitro dissolution of ACV from tablets was influenced by the swelling behaviour of each polymer. All data release of the studied tablets fitted to Hopfenberg model, which describes drug release from tablets displaying heterogeneous erosion. HPMC and CS/HPMC tablets revealed a sustained release for 24 h, but a complete dissolution of the tablets was not produced at this time. On the contrary, tablets which contained only CS as polymer were able to release the total amount of ACV for 4 h, due to the CS imbibition and erosion processes in pH 1.5 medium. These results allowed us to conclude that CS is the excipient to be chosen to obtain gastroretentive formulations, due to its demonstrated gastric compatibility.Key words acyclovir; chitosan; hydroxypropyl-methylcellulose; mucoadhesivity; drug controlled release; swelling behaviourIn recent years, the excipients choice for drug formulation has focused on natural and biocompatible products. Chitosan (CS) is a biocompatible material obtained from an abundant natural polysaccharide like chitin by deacetylation processes. 1)Several excellent reviews have compiled different methods for obtaining a wide range of chitosans with different deacetylation degrees and molecular weights which affect some of their physico-chemical parameters.2-4) In pharmaceutical technology field CS has found applicability as a potential formulation excipient acting as a disintegrant, binder or tablet coating agent. This polymer presents a swelling ability when it is placed within an aqueous media, 5) and mucoadhesivity in the oral cavity [6][7][8] and in the gastrointestinal tract. 9) CS is a well-known polycation that reacts with negatively charged components, either ions or molecules, leading to the formation of polyelectrolyte complex through ionic bridges between polymer chains. Their mucoadhesive property is mainly based on the ionic interaction with anionic substructures of mucous layer. 10)Hydroxypropyl-methylcellulose (HPMC) is a non-ionic cellulose ether which has methoxylic and hydroxypropoxylic moieties substituted onto the glucose units. Types of HPMC differ by various degrees of substitution of hydroxypropyl (hydrophilic) and methoxy (hydrophobic) groups and hence its versatility to retard drug release of various solubilities due to the ratio of hydroxypropyl to methoxyl content affects the extent of polymer interaction with water.11) This cellulose ether is the hydrophilic and swellable polymer most commonly used for the preparation of oral controlled drug delivery systems. [12][13][14] Upon contact wit...

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Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

Cited by 109 publications

References 13 publications

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

Sugar-based novel niosomal nanocarrier system for enhanced oral bioavailability of levofloxacin

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

Mucoadhesive Tablets for Controlled Release of Acyclovir

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