Evaluation of alternative strategies to optimize ketorolac transdermal delivery

Puglia, Carmelo; Filosa, Rosanna; Peduto, Antonella; Caprariis, P. De; Rizza, Luisa; Bonina, Francesco; Blasi, Paolo

doi:10.1208/pt070364

Cited by 76 publications

(44 citation statements)

References 33 publications

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“…The retentivity profile could be attributed to occlusive and bioadhesive properties of SLN, where occlusion decreases the transepidermal water loss, which further increases skin hydration and permeability. Further, it may also lead to accumulation of bioactives into the upper skin layers, reducing drug flux and creating a reservoir able to prolong skin residence time (Puglia et al, 2006), and, hence, could provide better treatment to upper skin infections and disorders. Similar results for MN skin permeation and deposition were obtained by 500 nm Peira et al 2008) using a microemulsion-based vehicle for topical delivery.…”

Section: In Vitro Skin Permeation Stripping and Retentivity Studiesmentioning

confidence: 99%

Design and development of solid lipid nanoparticles for topical delivery of an anti-fungal agent

Jain

Khare

et al. 2010

Drug Delivery

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Section: In Vitro Skin Permeation Stripping and Retentivity Studiesmentioning

confidence: 99%

Design and development of solid lipid nanoparticles for topical delivery of an anti-fungal agent

Jain

Khare

et al. 2010

Drug Delivery

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“…Enhancement of chemical stability after incorporation into lipid nanocarriers was proven for many cosmetic actives, e.g. coenzyme Q10 [164][165][166], ascorbyl palmitate [164,167], tocopherol (vitamin E) [165] and retinol (vitamin A) [168][169][170].…”

Section: Applications Of Nanocarrier Systems In Topical/transdermal Dmentioning

confidence: 99%

Nanocarrier Systems for Transdermal Drug Delivery

Escobar-Chávez¹,

Rodríguez-Cruz²,

Domínguez-Delgado³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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is an open discussion, in one hand, the nanotechnologist continue making new and more sophisticated nanocarriers and in the other hand, toxicologist continue evaluating possible damaging effects.Whatever it happens, nanotechnology is the new era and nanomedicine cannot be taking off. New nanocarriers will be created and the entire scientist working in nanomedicine bet for it to be the cure of diseases that in this moment are difficult to deal with [3] The application of preparations to the skin for medical purposes is as old as the history of medicine itself, with references to the use of ointments and salves found in the records of Babylonian and Egyptian medicine. The historical development of permeation research is well described by Hadgraft & Lane [4]. Over time, the skin has become an important route for drug delivery in which topical, regional or systemic effects are desired. Nevertheless, skin constitutes an excellent barrier and presents difficulties for the transdermal delivery of therapeutic agents, since few drugs possess the characteristics required to permeate across the stratum corneum in sufficient quantities to reach a therapeutic concentration in the blood. In order to enhance drug transdermal absorption different methodologies have been investigated developed and patented [5,6]. Improvement in physical permeationenhancement technologies has led to renewed interest in transdermal drug delivery. Some of these novel advanced transdermal permeation enhancement technologies include: iontophoresis, electroporation, ultrasound, microneedles to open up the skin and more recently the use of transdermal nanocarriers [3,[7][8][9][10].A number of excellent reviews that have been published contain detailed discussions concerning many aspects of transdermal nanocarriers [11][12][13][14][15][16][17]. The present chapter shows an updated overview of the use of submicron particles and other nanostructures in the pharmaceutical field, specifically in the area of topical and transdermal drugs. This focus is justified due to the magnitude of the experimental data available with the use of these nanocarriers. The development of submicron particles and other nanostructures in the pharmaceutical and cosmetic fields has been emerged in the last decades for designing best formulations for application through the skin [18][19][20][21]. The skinThe skin is the largest organ of the body [22][23][24], accounting for more than 10% of body mass, and the one that enables the body to interact more intimately with its environment. Essentially, the skin consists of four layers: The SC, that is the outer layer of the skin (nonviable epidermis), and forms the rate-controlling barrier for diffusion for almost all compounds. It is composed of dead flattened, keratin-rich cells, the corneocytes. These dense cells are surrounded by a complex mixture of intercellular lipids, namely, ceramides, free fatty acids, cholesterol, and cholesterol sulphate. Their most important feature is that they are structured as ordered bilayer arrays [25]...

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“…Additionally, high analgesic activity and low molecular weight of ketorolac make it a good candidate for transdermal delivery. Several transdermal delivery strategies such as use of permeation enhancers [6], proniosomes [7], its prodrugs [8], iontophoresis [9], ultrasound [10], cyclodextrins and liposomes [11], and nanostructured lipid carriers (NLCs) [12] have been developed so far. The present study aims to prepare and characterize nanoparticle of ketorolac tromethamine with RS-100 and RL-100 as polymers to enhance dissolution and bioavailability of the drug.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Ketorolac Tromethamine Nanoparticle with Eudragit RS-100 and RL-100 by Nano precipitation Method

2017

International Journal of Research in Pharmacy and Biosciences

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Nano-carriers with optimized physicochemical and biological properties are taken up by cells more easily than larger molecules, so they can be successfully used as delivery tools for currently available bioactive compounds.Nanoparticles of Ketorolac tromethamine, a potent analgesic and moderate anti-inflammatory activitywith eudragit RS-100 and RL-100 for enhance dissolution and bioavailability of the drug by nanoprecipitation method. SEM studies on optimized formulations (F3, F6) were conducted. Partition coefficient (2.2), particle size (0.276 ±0.015 to 1.236 ±0.115nm), zeta potential (+32.5±1.2 to +42.3±2.9 mV), drug content (70.196 ± 8.26 to 95.882 ± 15.33%), drug release kinetic studies best fitted to zero order release. Size range of all the batches was within 500 nm with polydispersity index of 0.4 to 0.6. Additionally, SEM images showed almost spherical particles with smooth surface were obtained. No major drug polymer interaction was detected using FTIR, DSC, PXRD studies done for solid state characterization. Drug encapsulation efficiency was found to be in the range of 75% to 95% which is high due to the solubility of ketorolac. In terms of Encapsulation efficiency, batch F3 and F6 showed relatively higher drug Encapsulation efficiency. The percentage yield of all the formulations ranged between 27-42%. All the batches showed sustained drug release profile. The percentage release for all the formulations ranged from 70-93% for all the formulations after 12 h. Short term stability studies of around two months revealed stable nanoparticle with no significant change in drug content.

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Evaluation of alternative strategies to optimize ketorolac transdermal delivery

Cited by 76 publications

References 33 publications

Design and development of solid lipid nanoparticles for topical delivery of an anti-fungal agent

Design and development of solid lipid nanoparticles for topical delivery of an anti-fungal agent

Nanocarrier Systems for Transdermal Drug Delivery

Formulation and Characterization of Ketorolac Tromethamine Nanoparticle with Eudragit RS-100 and RL-100 by Nano precipitation Method

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