Development of O/W nanoemulsions for ophthalmic administration of timolol

Gallarate, Marina; Chirio, Daniela; Bussano, Rosanna; Peira, Elena; Battaglia, Luigi; Baratta, Francesca; Trotta, Michele

doi:10.1016/j.ijpharm.2012.10.015

Cited by 72 publications

(52 citation statements)

References 30 publications

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“…From a technological point of view, increasing the amphiphilic or lipophilic character of a drug can improve its encapsulation in lipid-based nanocarriers, thus allowing to take the advantages deriving from the in vivo administration of colloidal delivery system [22][23][24][25] . In this study, a lipophilic prodrug of LHRH, suitably linked to CF for imaging purposes, was associated to liposomal systems with various composition, charge and lamellarity.…”

Section: Resultsmentioning

confidence: 99%

A study on liposomal encapsulation of a lipophilic prodrug of LHRH

Pignatello

Musumeci

Graziano

et al. 2015

Pharmaceutical Development and Technology

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This study aimed at evaluating whether derivatization of luteinizing hormone-releasing hormone (LHRH) peptide with an amphiphilic lipoamino acid moiety could allow, along with other technological and/or pharmacokinetic advantages, to improve its encapsulation in liposomes, potentially driving its further body distribution and cellular uptake. Experimental data confirmed that a lipophilic derivative of LHRH was efficiently incorporated in various liposomal systems, differing in lipid composition and surface charge, and obtained using different methods of production. Incubation of liposomes, loaded with a fluorescent derivative of the LHRH prodrug, with NCTC keratinocytes or Caco-2 cell cultures showed that the carriers can be rapidly internalized. Conversely, the internalization of the free prodrug occurred only at very high concentrations.

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Section: Resultsmentioning

confidence: 99%

A study on liposomal encapsulation of a lipophilic prodrug of LHRH

Pignatello

Musumeci

Graziano

et al. 2015

Pharmaceutical Development and Technology

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“…For example, a nanoemulsion containing indomethacin coated with chitosan showed a higher distribution on the ocular surface and a higher concentration of indomethacin in the cornea (1.6‐fold), conjunctiva (1.4‐fold) and aqueous humour (1.8‐fold) after topical instillation in rabbits than a non‐chitosan‐coated nanoemulsion . A chitosan nanoemulsion containing timolol maleate coated with bis(2‐ethylexyl‐sulfosuccinate) and chitosan (0.5%) showed a sixfold improvement in drug permeation into the cornea relative to the same formulation without chitosan . Moreover, the attraction of positively charged nanodroplets to the cornea was reported by Hagigit et al ., who used a cationic nanoemulsion containing DOTAP to deliver an antisense oligonucleotide.…”

Section: Delivery Systemsmentioning

confidence: 99%

“…[96,97,112] To obtain positively charged nanoemulsions, cationic polymers and surfactants are generally used. The most frequently studied species are chitosan, [41][42][43]45,111] 1,2-dioleoyl-3-trimethylammonium-propane chloride (DOTAP) [34,36,37] and quaternary ammoniums. [35] For example, a nanoemulsion containing indomethacin coated with chitosan showed a higher distribution on the ocular surface and a higher concentration of indomethacin in the cornea (1.6fold), conjunctiva (1.4-fold) and aqueous humour (1.8fold) after topical instillation in rabbits than a nonchitosan-coated nanoemulsion.…”

Section: Concentration (Maximum Potency) Referencesmentioning

confidence: 99%

Topical delivery of ocular therapeutics: carrier systems and physical methods

Souza

Dias

Pereira

et al. 2013

Journal of Pharmacy and Pharmacology

115

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Objective The basic concepts, major mechanisms, technological developments and advantages of the topical application of lipid-based systems (microemulsions, nanoemulsions, liposomes and solid lipid nanoparticles), polymeric systems (hydrogels, contact lenses, polymeric nanoparticles and dendrimers) and physical methods (iontophoresis and sonophoresis) will be reviewed. Key findings Although very convenient for patients, topical administration of conventional drug formulations for the treatment of eye diseases requires high drug doses, frequent administration and rarely provides high drug bioavailability. Thus, strategies to improve the efficacy of topical treatments have been extensively investigated. In general, the majority of the successful delivery systems are present on the ocular surface over an extended period of time, and these systems typically improve drug bioavailability in the anterior chamber whereas the physical methods facilitate drug penetration over a very short period of time through ocular barriers, such as the cornea and sclera. Summary Although in the early stages, the combination of these delivery systems with physical methods would appear to be a promising tool to decrease the dose and frequency of administration; thereby, patient compliance and treatment efficacy will be improved.

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“…Furthermore, they can be exploited for image-guided drug delivery by utilizing targeting and imaging components (7,13). They are also being investigated widely for potential applications in transdermal delivery (11), ophthalmic (14), and pulmonary (15) drug delivery.…”

Section: Introduction-applications Of Nanoemulsions In Drug Deliverymentioning

confidence: 99%

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

et al. 2014

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Abstract. Nanoemulsion dosage form serves as a vehicle for the delivery of active pharmaceutical ingredients and has attracted great attention in drug delivery and pharmacotherapy. In particular, nanoemulsions act as an excellent vehicle for poorly aqueous soluble drugs, which are otherwise difficult to formulate in conventional dosage forms. Nanoemulsions are submicron emulsions composed of generally regarded as safe grade excipients. Particle size at the nanoscale and larger surface area lead to some very interesting physical properties that can be exploited to overcome anatomical and physiological barriers associated in drug delivery to the complex diseases such as cancer. Along these lines, nanoemulsions have been engineered with specific attributes such as size, surface charge, prolonged blood circulation, target specific binding ability, and imaging capability. These attributes can be tuned to assist in delivering drug/imaging agents to the specific site of interest, based on active and passive targeting mechanisms. This review focuses on the current state of nanoemulsions in the translational research and its role in targeted cancer therapy. In addition, the production, physico-chemical characterization, and regulatory aspects of nanoemulsion are addressed.

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Development of O/W nanoemulsions for ophthalmic administration of timolol

Cited by 72 publications

References 30 publications

A study on liposomal encapsulation of a lipophilic prodrug of LHRH

A study on liposomal encapsulation of a lipophilic prodrug of LHRH

Topical delivery of ocular therapeutics: carrier systems and physical methods

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

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