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1.
Ther Deliv ; 2024 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-38180042

RESUMO

Aim: This investigation aimed to develop a voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat fungal keratitis. Methods: Microemulsions were prepared using water titration, and the optimized microemulsion was coated with chitosan to prepare CVME. The physicochemical parameters, ocular irritation potential, in vitro antifungal efficacy and in vitro release studies were performed. The in vivo antifungal efficacy study was conducted in a fungal infection-induced rabbit eye model. Results: The developed CVME displayed acceptable physicochemical properties and excellent mucoadhesive behavior and showed a sustained release profile. Ex vivo and in vivo studies concluded that higher permeability and improved antifungal efficacy were observed for CVME than drug suspension (DS). Conclusion: The prepared CVME7 is a viable alternative to treating fungal keratitis with existing approaches.


Nanotechnology can help resolve problems that are currently associated with eye medications. Microemulsions (MEs) are mixtures containing tiny droplets of oil and water, which are made stable by ingredients called surfactants (meaning a type of soap) and co-surfactants. The ability for medications to be released slowly in MEs makes them suitable for eye medications because they reduce the number of times eye drops need to be used each day. This study wanted to create a medicine called voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat a fungal infection in the eye called keratitis. We made MEs by gradually adding a combination of oil, surfactant, and water together. Then, we coated the best MEs with a substance called chitosan to make CVME. We tested its physical and chemical properties, whether it irritated the eyes, how well it could fight fungus, and how it released medicine. We tested CVME on rabbits with a fungal eye infection. CVME had good physical and chemical properties and stuck well to the mucus on the surface of the eyes. It released the medicine slowly. The system created in this study is very important for treating fungal infections because it helps the medicine stay on the eye surface longer and allows it to better reach the infected areas of the eye. CVME7 might be a better option for treating fungal keratitis instead of other methods that are currently used.

2.
Curr Eye Res ; 47(11): 1498-1507, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-36099026

RESUMO

PURPOSE: Moxifloxacin (MOX) is a fourth-generation fluoroquinolone and a broad spectrum antibiotic used in the management of bacterial keratitis (BK). This investigation aimed to formulate MOX-loaded chitosan/pectin cationic polyelectrolyte nanocapsules (CPNCs) for the effective topical treatment of BK. METHODS: Physicochemical properties like nanocapsule size, charge, drug entrapment efficiency (EE), viscosity, pH, and in-vitro release profile of CPNCs were evaluated. The in-vitro antibacterial activity of CPNCs and marketed formulations (MFs) was studied against Staphylococcus aureus. Ex-vivo corneal permeation studies of CPNCs were evaluated with the help of a modified diffusion apparatus, which was used with goat cornea. The pharmacodynamic study was performed with optimized CPNCs on a BK-induced rabbit eye model and compared with MF. RESULTS: The optimized nanocapsules appeared as positive charge (+19.91 ± 0.66) with a nano size (242.0 ± 0.30 nm) as calculated by the dynamic light scattering method. The in-vitro release profile of CPNCs exhibited sustained release properties. The ex-vivo permeation pattern also supported the improved drug permeation through the cornea from CPNCs as compared with MF. Draize irritation studies confirmed that the prepared formulation is compatible with the corneal tissue. The in-vivo study concluded that the antibacterial activity of CPNCs was improved when evaluated with MF. CONCLUSION: The obtained results showed that CPNCs were the better choice for the management of BK therapy due to its capability to improve the corneal adhesion of CPNCs through direct interaction with the mucous membrane of the corneal tissue.


Assuntos
Quitosana , Ceratite , Nanocápsulas , Animais , Antibacterianos , Quitosana/química , Córnea , Preparações de Ação Retardada , Fluoroquinolonas , Moxifloxacina/química , Tamanho da Partícula , Pectinas , Polieletrólitos , Coelhos
4.
Arch Microbiol ; 204(7): 416, 2022 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-35737130

RESUMO

Enterocytozoon hepatopanaei parasite (EHP) is identified as an emerging pathogenic microsporidium parasite in shrimp culture industry. Though the etiology, disease pattern and sustainability of shrimp are well known, significantly less research has been carried out about the disease transmission and symptoms of infected aquatic animals. The present study aims is to determine the disease carrier status of five different species of Indian marine crabs (Scylla olivacea, Scylla serrata, Portunus pelagicus, Ocypode quadrata and Portunus sanquinolentus) using EHP. At the first instance, oral infection and intramuscular injection were performed to determine the susceptibility of the parasite at 50 days post-infection and it was observed that there was no mortality. The experimental infected crabs were confirmed by polymerase chain reaction, bioassay and histopathology. The crabs were EHP-PCR positive at 5th day post-infection (d.p.i) in gills, heart, hepatopancreas, haemolymph and muscle tissue. However, after 5th d.p.i EHP was PCR negative in all the tissue samples. There were no mortalities and histological changes in the negative group and experimental group. Therefore, marine crabs are found to be not suitable hosts for replicating EHP spores but crabs fecal matters are PCR positive till 5th d.p.i. Therefore, marine crabs are having the possibilities of acceptance as a vector for Enterocytozoon hepatopanaei in shrimp. Shrimp farmers need to take necessary action to control this deadly infection in shrimp ponds.


Assuntos
Braquiúros , Enterocytozoon , Parasitos , Penaeidae , Animais , Enterocytozoon/genética , Hepatopâncreas
5.
Curr Eye Res ; 46(12): 1844-1852, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34176380

RESUMO

Purpose: The aim of this study was to formulate brimonidine tartrate loaded phase transition microemulsions (PMEs), which undergo phase transition from water in oil (W/O) microemulsions to liquid crystalline (LC) and then oil in water (O/W) microemulsions after instilled into the eye and prolong the precorneal residence time and ocular bioavailability for the effective treatment of glaucoma.Methods: The pseudo-ternary phase diagram was developed and various PMEs were prepared using Tween 80 and Span 80 with isopropyl myristate and water. Globule size and shape, physicochemical parameters, in vitro and ex vivo drug release of PMEs were studied. The in vivo anti-glaucoma efficacy of optimized PMEs was studied in an experimental rabbit eyes model and compared with marketed formulation (MF).Results: Globule size of PMEs was found less than 200 nm, which was confirmed by both dynamic light scattering technique and Transmission Electron Microscopy. Physicochemical properties such as pH, refractive index, percentage transparency, viscosity and conductivity were also found in the acceptable ranges. In vitro release studies of PMEs exhibited sustained release property. Ex vivo permeation study also supported the enhanced drug flux through cornea from PMEs as compared with MF. In pharmacodynamic study, a greater reduction in intraocular pressure was seen in PMEs as compared to MF.Conclusion: PMEs as ocular drug delivery system offer a promising approach to enhance the corneal contact, higher permeation and prolonged precorneal retention time in the eye leading to sustained drug release, enhanced bioavailability and patient compliance.


Assuntos
Tartarato de Brimonidina/farmacocinética , Córnea/efeitos dos fármacos , Sistemas de Liberação de Medicamentos/métodos , Glaucoma/tratamento farmacológico , Agonistas de Receptores Adrenérgicos alfa 2/farmacocinética , Animais , Córnea/metabolismo , Modelos Animais de Doenças , Liberação Controlada de Fármacos , Emulsões/farmacocinética , Glaucoma/metabolismo , Glaucoma/fisiopatologia , Cabras , Pressão Intraocular/efeitos dos fármacos , Tamanho da Partícula , Coelhos
6.
AAPS PharmSciTech ; 22(5): 195, 2021 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-34184117

RESUMO

Microbial keratitis (MK) is a vision-threatening disease and the fourth leading cause of blindness worldwide. In this work, we aim to develop moxifloxacin (MXN)-loaded chitosan-based cationic mucoadhesive polyelectrolyte nanocapsules (PENs) for the effective treatment of MK. PENs were formulated by polyelectrolyte complex coacervation method and characterized for their particle size, surface charge, morphology, mucoadhesive property, in-vitro and ex-vivo release, ocular tolerance, and antimicrobial efficacy studies. The pharmacodynamic study was conducted on rabbit eye model of induced keratitis and it is compared with marketed formulation (MF). Developed PENs showed the size range from 230.7 ± 0.64 to 249.0 ± 0.49 nm and positive surface charge, spherical shape along with appropriate physico-chemical parameters. Both in-vitro and ex-vivo examination concludes that PENs having more efficiency in sustained release of MXN compared to MF. Ocular irritation studies demonstrated that no corneal damage or ocular irritation. The in-vivo study proved that the anti-bacterial efficacy of PENs was improved when compared with MF. These results suggested that PENs are a feasible choice for MK therapy because of their ability to enhance ocular retention of loaded MXN through interaction with the corneal surface of the mucous membrane.


Assuntos
Desenvolvimento de Medicamentos/métodos , Ceratite/tratamento farmacológico , Moxifloxacina/síntese química , Nanocápsulas/química , Polieletrólitos/síntese química , Animais , Antibacterianos/administração & dosagem , Antibacterianos/síntese química , Antibacterianos/farmacocinética , Embrião de Galinha , Córnea/efeitos dos fármacos , Córnea/metabolismo , Córnea/microbiologia , Cabras , Ceratite/metabolismo , Ceratite/microbiologia , Moxifloxacina/administração & dosagem , Moxifloxacina/farmacocinética , Nanocápsulas/administração & dosagem , Polieletrólitos/administração & dosagem , Polieletrólitos/farmacocinética , Coelhos
7.
Curr Pharm Des ; 26(42): 5518-5532, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32938345

RESUMO

Topical ocular delivery is an acceptable and familiar approach for the treatment of common ocular diseases. Novel strategies for the treatment of inherited eye diseases include new pharmacologic agents, gene therapy and genome editing, which lead to the expansion of new management options for eye disorders. The topical ocular delivery of nanocarriers is a technique, which has the potential to facilitate novel treatments. Nanocarrier- based strategies have proven effective for site-targeted delivery. This review summarizes recent development in the area of topical delivery of different nanocarriers (Polymer, Vesicular and dispersed systems) for the management of glaucoma, a group of ocular disorders characterized by progressive and accelerated degeneration of the axons of retinal ganglion cells, which make up the optic nerve. Unique cellular targets for glaucoma treatment, primarily the trabecular meshwork of the anterior segment of the eye, make glaucoma facilitated by the use of nanocarriers an ideal disorder for novel molecular therapies.


Assuntos
Glaucoma , Pressão Intraocular , Glaucoma/tratamento farmacológico , Humanos , Células Ganglionares da Retina , Malha Trabecular
8.
Int J Biol Macromol ; 152: 1224-1232, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31751741

RESUMO

AIM: Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. The aim of this study was to prepare BNZ loaded chitosan-pectin mucoadhesive nanocapsules (CPNCs) by polyelectrolyte complex coacervation method for ocular delivery and evaluated for its anti glaucoma efficacy. METHODS: The prepared CPNCs were characterized for their particle size, polydispersity index, zeta-potential, surface morphology, entrapment efficiency, drug loading efficiency, mucoadhesive strength in-vitro and ex-vivo release. The pharmacodynamic studies were conducted for CPNCs on glaucoma induced rabbit eye model and compared with marketed product. RESULT AND DISCUSSION: All the formulated CPNCs exhibited the size range from 217.01 ± 0.21 to 240.05 ± 0.08 nm and appropriate physico-chemical parameters, and depicted a couple of erosion- diffusion release of BNZ over a time of 8 h. Ex-vivo corneal permeation study concluded that BNZ loaded CPNCs crosses the cornea potentially higher rate as compared to the marketed product. In pharmacodynamic study, greater intraocular pressure lowering effect was achieved by CPNCs as compared to marketed drug product. CONCLUSION: The result concluded that CPNCs are a feasible choice to conventional eye drops because of its ability to improve the bioavailability via its longer precorneal retention time and its ability to sustained release of the drug.


Assuntos
Quitosana/química , Glaucoma/tratamento farmacológico , Nanocápsulas/química , Pectinas/química , Sulfonamidas/química , Sulfonamidas/farmacologia , Tiazinas/química , Tiazinas/farmacologia , Animais , Disponibilidade Biológica , Inibidores da Anidrase Carbônica/química , Inibidores da Anidrase Carbônica/farmacologia , Córnea/efeitos dos fármacos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Pressão Intraocular/efeitos dos fármacos , Nanopartículas/química , Soluções Oftálmicas/química , Soluções Oftálmicas/farmacologia , Tamanho da Partícula , Polieletrólitos/química , Polieletrólitos/farmacologia , Coelhos
9.
Ocul Immunol Inflamm ; 27(2): 303-311, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-28910554

RESUMO

PURPOSE: The purpose of this study was to investigate the self-microemulsifying drug delivery systems (SMEDDS) for ophthalmic delivery of Prednisolone (PDN) to treat uveitis. MATERIALS AND METHODS: The pseudo-ternary phase diagrams were developed, and various SMEDDS were prepared using Linoleic acid as oil, Cremophore RH 40 as a surfactant, and propylene glycol as a co-surfactant. Physicochemical parameters (globule size, zeta potential, viscosity, and pH) and in vitro release of SMEDDS were studied. The in vivo efficacy of prepared formulations and the marketed drug solution was studied by administering them topically to an endotoxin-induced uveitis rabbit model. RESULTS: All formulations displayed an average globule size less than 100 nm. The developed SMEDDS exhibited acceptable physicochemical behavior and displayed sustained drug release. In vivo studies in a rabbit eye showed a marked improvement in the anti-inflammatory activity of developed formulation compared with a marketed formulation in a uveitis-induced rabbit eye model. CONCLUSIONS: The developed SMEDDS are a feasible option to conventional eye drops for its capability to improve bioavailability via its longer precorneal residence time and its capacity to sustain the release of the drug.


Assuntos
Sistemas de Liberação de Medicamentos , Prednisolona/administração & dosagem , Uveíte/tratamento farmacológico , Animais , Modelos Animais de Doenças , Emulsões , Glucocorticoides/administração & dosagem , Soluções Oftálmicas , Coelhos , Uveíte/patologia
10.
J Microencapsul ; 35(3): 292-300, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29771175

RESUMO

The objective of this study was to evaluate the potential of chitosan-gellan nanocapsules (CGNCs) for encapsulation and sustained release of Tamoxifen citrate (TMC) for breast cancer therapy. Polyelectrolyte complex coacervation method was used for production of CGNCs. Interaction studies were conducted by Fourier-transform infra-red (FT-IR), differential scanning colorimetric (DSC), and X-ray diffraction (XRD) to investigate any interaction between drug and excipients. Physicochemical parameters, in vitro drug release and release kinetic were studied. In vitro cell viability study using Michigan Cancer Foundation-7 (MCF-7) breast cancer cells was also investigated. CGNCs had a smooth surface and nanosize range with a positive surface charge and exhibited sustained drug release. Further, TMC loaded CGNCs were found to be more cytotoxic than the free drug in MCF-7. Thus CGNCs may be suitable for breast cancer treatment due to delivering the drug at the site of action for a prolonged period of time.


Assuntos
Antineoplásicos Hormonais/administração & dosagem , Neoplasias da Mama/tratamento farmacológico , Quitosana/química , Nanocápsulas/química , Polissacarídeos Bacterianos/química , Tamoxifeno/administração & dosagem , Antineoplásicos Hormonais/química , Antineoplásicos Hormonais/farmacocinética , Antineoplásicos Hormonais/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Feminino , Humanos , Células MCF-7 , Tamoxifeno/química , Tamoxifeno/farmacocinética , Tamoxifeno/farmacologia
11.
Ther Deliv ; 8(5): 313-330, 2017 03.
Artigo em Inglês | MEDLINE | ID: mdl-28361605

RESUMO

Microemulsions (MEs) are thermodynamic stable dispersion of oily phase and aqueous phase stabilized by surfactants and co-surfactants, and are a small droplet size of less than 100 nm. MEs are appropriate systems for ocular drug delivery because they improve ocular drug retention, extended duration of action, high ocular absorption, permeation of loaded drugs and effortlessness of preparation and administration. This review is an effort to summarize the recent development in the area of MEs, self-emulsifying drug delivery systems, which are examined in relation to their uses in ocular drug delivery. The noteworthy patent, toxicity and stability issues related to these ME systems are also explored here.


Assuntos
Administração Oftálmica , Sistemas de Liberação de Medicamentos , Emulsões/administração & dosagem , Humanos , Óleos , Tensoativos , Água
12.
Ocul Immunol Inflamm ; 25(4): 463-474, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26943481

RESUMO

PURPOSE: Moxifloxacin (MXN) is widely prescribed for the treatment of bacterial keratitis. The conventional MXN solution has several limitations, including short precorneal residence time and poor intrastromal bioavailability, requiring frequent instillation of the drug to achieve the desired therapeutic effect. To circumvent this problem, the W/O (water-in-oil) microemulsion (ME) system was utilized for sustained release and improved precorneal retention. METHODS: The pseudo-ternary phase diagrams were developed and various MEs were prepared using two non-ionic surfactants, Tween 80 and Span 20, with isopropyl myristate and acetate buffer. Physicochemical parameters, in vitro drug release and in vitro antibacterial activity were studied. The in vivo antimicrobial efficacy of optimized microemulsion (ME 10) was studied in an experiment on bacterial keratitis in rabbit eyes and compared with that of the marketed eye drops. RESULTS: The optimized microemulsion (ME 10) displays as an average globule size of <40 nm. The developed MEs showed acceptable physico-chemical behaviour, good stability for 3 months and exhibited sustained drug release. Greater efficacy in experimental bacterial keratitis in rabbit eyes was also observed in comparison with marketed drug solution. CONCLUSIONS: The developed MEs are a viable alternative to conventional eye drops, because of its ability to enhance bioavailability through its longer precorneal residence time and its ability to sustain the release of the drug.


Assuntos
Úlcera da Córnea/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Emulsões/química , Infecções Oculares Bacterianas/tratamento farmacológico , Fluoroquinolonas/administração & dosagem , Transição de Fase , Infecções Estafilocócicas/tratamento farmacológico , Animais , Antibacterianos/administração & dosagem , Antibacterianos/química , Antibacterianos/farmacocinética , Úlcera da Córnea/microbiologia , Escherichia coli/efeitos dos fármacos , Infecções Oculares Bacterianas/microbiologia , Fluoroquinolonas/química , Hexoses/química , Microscopia Eletrônica de Transmissão , Moxifloxacina , Miristatos/química , Óleos/química , Tamanho da Partícula , Polissorbatos/química , Coelhos , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Água/química
13.
Pharm Dev Technol ; 22(4): 617-626, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27574791

RESUMO

Clotrimazole (CTZ) is a broad spectrum antimycotic agent known to be very effective locally for the treatment of fungal skin infections. The aim of this study was to study the effect of chitosan-coated microemulsion (CME) for topical delivery of CTZ and also evaluate its in vitro antifungal efficacy, ex vivo permeation and retention ability on the skin surface. The pseudo-ternary phase diagrams were developed using clove oil as oil phase, Tween 80 and propylene glycol as surfactant and co-surfactant, respectively, and distilled water as aqueous phase. CME was prepared by the drop wise addition of chitosan solution to the optimized microemulsion. Physicochemical parameters (globule size, zeta potential, drug content, viscosity and pH) and in vitro release of CME were studied. The in vitro antifungal efficacy of CME and ME was studied by cup-plate method against Candida albicans. Ex vivo drug permeation study was also carried out in a modified diffusion cell, using rat skin. The developed CME displayed an average globule size less than 50 nm and a positive surface charge, acceptable physico-chemical behavior, and exhibited sustained drug release in in vitro study. In in vitro anti-fungal study, CME showed greater values of zone of inhibition as compared to ME due to its prolonged action as well as fungistatic nature of chitosan. In ex vivo study, CME showed better retention and sustained permeation property than ME due to the mucoadhesive property of chitosan. These results suggest that positively charged CMEs could be used as novel topical formulation for its ability to retain on the skin and its ability to sustain the release of the drug.


Assuntos
Anti-Infecciosos Locais/administração & dosagem , Anti-Infecciosos Locais/farmacocinética , Quitosana/química , Clotrimazol/administração & dosagem , Clotrimazol/farmacocinética , Emulsões/química , Administração Cutânea , Animais , Anti-Infecciosos Locais/farmacologia , Antifúngicos/administração & dosagem , Antifúngicos/farmacocinética , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Candidíase/tratamento farmacológico , Clotrimazol/farmacologia , Tamanho da Partícula , Transição de Fase , Ratos Wistar
14.
Ocul Immunol Inflamm ; 24(5): 489-92, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26133969

RESUMO

PURPOSE: To investigate the therapeutic effectiveness of ion-activated mucoadhesive hydrogel system in the treatment of experimental bacterial keratitis. MATERIALS AND METHODS: Mucoadhesive systems were prepared using gellan or sodium alginate alone and combined with sodium carboxymethylcellulose (NaCMC) to enhance the gel bioadhesion properties. The in vivo antimicrobial efficacy of selected mucoadhesive systems was studied in an experiment on bacterial keratitis in rabbit's eyes and compared with that of the marketed conventional eyedrops. RESULTS: Ocular tolerance was studied in the eye of albino rabbits and tested formulations were non-irritant with no sign of inflammation. Better improvement in experimental bacterial keratitis in rabbit eyes was observed in animals treated with mucoadhesive hydrogel formulation (GG5 and GS5) compared with marketed drug solution. CONCLUSION: The developed system is a viable alternative to conventional eyedrops of GTN due to its ability to enhance bioavailability through its longer precorneal residence time.


Assuntos
Antibacterianos/administração & dosagem , Úlcera da Córnea/tratamento farmacológico , Modelos Animais de Doenças , Portadores de Fármacos , Infecções Oculares Bacterianas/tratamento farmacológico , Fluoroquinolonas/administração & dosagem , Hidrogéis/administração & dosagem , Infecções Estafilocócicas/tratamento farmacológico , Alginatos/química , Animais , Disponibilidade Biológica , Carboximetilcelulose Sódica/química , Química Farmacêutica , Úlcera da Córnea/microbiologia , Infecções Oculares Bacterianas/microbiologia , Gatifloxacina , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Hidrogéis/química , Polissacarídeos Bacterianos/química , Coelhos , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Resultado do Tratamento
15.
Ther Deliv ; 4(11): 1385-95, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24228989

RESUMO

BACKGROUND: The objective of this investigation was to evaluate the potential of mucoadhesive chitosan-coated positively charged microemulsions (CH-MEs) of dexamethasone with respect to the change in nonionic cosurfactants. METHODS: CH-MEs were prepared with different concentrations of surfactant and cosurfactant using the water titration method and coated with low-molecular-weight chitosan. RESULTS: All formulations displayed an average globule size between 85 and 187 nm and a positive surface charge. The optimized CH-MEs showed greater penetration of dexamethasone in the anterior segment of the eye, resulting in twofold and fourfold higher dexamethasone concentration than uncoated ME and drug suspension, respectively. CONCLUSION: The developed CH-MEs shows increases in ocular penetration and bioavailability.

16.
Expert Opin Drug Deliv ; 10(1): 5-15, 2013 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23106236

RESUMO

OBJECTIVES: The objective of this study is to develop stable, biodegradable chitosan-sodium alginate-based dual, ionic cross-linked multiparticulate system (microbeads) of tinidazole for targeted colon delivery and sustained drug release for the treatment of amoebiasis and thereby evaluating its targeting approach through in vivo gamma scintigraphic imaging technique. METHODS: The chitosan-sodium alginate-based multiparticulate system developed was producing sustained effect by virtue of its mechanical strength using double ionotropic gelation method utilizing calcium chloride and sodium sulfate as first and second cross-linkers respectively. Prepared formulations were evaluated for percent yield, drug entrapment efficiency, particle size, degree of swelling, in vitro kinetics, and in vivo targeting potentials using gamma scintigraphic imaging technique. RESULTS: The obtained particulates were spherical, free flowing, and had a mean particle size ranging from 1.422 mm to 1.881 mm, whereas percent yield and percent drug entrapment efficiency was found to be in between 72.61 to 82.43% and 63.25 to 79.32% respectively. CONCLUSION: The prepared multiparticulate system showed better sustained release property and in vivo ability to target colon for drug delivery. Hence, the developed multiparticulate system could be a promising device to achieve greater site-specificity to colon.


Assuntos
Alginatos/química , Antitricômonas/farmacocinética , Quitosana/química , Colo/metabolismo , Portadores de Fármacos , Tinidazol/farmacocinética , Animais , Antitricômonas/administração & dosagem , Química Farmacêutica , Colo/diagnóstico por imagem , Preparações de Ação Retardada , Sistemas de Liberação de Medicamentos/métodos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Masculino , Microesferas , Compostos de Organotecnécio , Tamanho da Partícula , Cintilografia , Compostos Radiofarmacêuticos , Ratos , Tinidazol/administração & dosagem
17.
Curr Eye Res ; 38(3): 342-52, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-23216079

RESUMO

PURPOSE: Dexamethasone (DXN) is an effective anti-inflammatory drug in the treatment of acute and chronic eye disease such as uveitis. However, its low aqueous solubility limits its clinical usefulness. The purpose of this study was to investigate the mucoadhesive chitosan-coated cationic microemulsions (CH-MEs) for ophthalmic delivery of DXN to treat uveitis. MATERIALS AND METHODS: The pseudo-ternary phase diagrams were developed and various MEs were prepared using isopropyl myristate as oil, Tween 80 as a surfactant, propylene glycol as a co-surfactant and distilled water. MEs were prepared and coated with chitosan by the dropwise addition of chitosan solution in the ME dispersion. Physicochemical parameters (globule size, zetapotential, drug content, viscosity, refractive index and pH), mucoadhesive properties and the in vitro release of MEs were studied. The in vivo efficacy of prepared formulations and the marketed drug solution were studied by administering them topically to endotoxin-induced uveitis rabbit model. RESULTS: All formulations displayed an average globule size less than 200 nm and a positive surface charge. The developed CH-MEs showed acceptable physico-chemical behavior, good mucoadhesive properties, good stability for three months and exhibited sustained drug release. In vivo studies in rabbit eye showed a marked improvement in the anti-inflammatory activity of mucoadhesive CH-ME-treated eye compared with a marketed suspension formulation in a uveitis-induced rabbit eye model. CONCLUSION: The developed CH-MEs are a viable alternative to conventional eye drops for its ability to enhance bioavailability through its longer precorneal residence time and its ability to sustain the release of the drug.


Assuntos
Quitosana/química , Dexametasona/administração & dosagem , Sistemas de Liberação de Medicamentos , Emulsões/química , Glucocorticoides/administração & dosagem , Uveíte/tratamento farmacológico , Animais , Humor Aquoso/metabolismo , Disponibilidade Biológica , Química Farmacêutica , Dexametasona/farmacocinética , Modelos Animais de Doenças , Estabilidade de Medicamentos , Glucocorticoides/farmacocinética , Microscopia Eletrônica de Transmissão , Mucina-2/química , Tamanho da Partícula , Poliaminas , Polieletrólitos , Polissorbatos/química , Propilenoglicol/química , Coelhos , Solubilidade , Uveíte/metabolismo , Viscosidade
18.
Asian Pac J Trop Med ; 4(8): 649-53, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21914545

RESUMO

OBJECTIVE: To evaluate the anti-inflammatory and analgesic activities of the ethanol and aqueous extracts of prop roots of Pandanus fascicularis (P. fascicularis) Lam (pandanaceae). And provide experimental evidence for its traditional use such as rheumatoid arthritis and spasmodic. METHODS: The anti-inflammatory activity was observed by carrageenan-induced edema of the hind paw of rats. Analgesic activities of prop roots of P. fascicularis were determined using acetic acid induced writhing model and tail clip method in mice and rat, respectively. The ethanol fraction was then subjected to chromatographic analysis and a compound has been isolated and characterized by IR, (1)H-NMR and mass spectroscopy. RESULTS: Edema suppressant effect of ethanol extract was found to be 37.03% inhibition whereas aqueous extract was found to be 63.22% inhibition after 3 h which was nearly equivalent to that of 10 mg/kg of indomethacin (67.81%). Percentage inhibition of writhing compared to control were 63.15%, 54.38%, 14.90% for aspirin, aqueous extract and ethanolic extract, respectively. Both ethanol and aqueous extracts show significant activity against appropriate controls after 60 min of treatment on tail clip method. The structure of the isolated compound is may be characterized as Hepta deca-5-ene-1-ol by analysis it's IR, (1)H-NMR and mass spectroscopy data. CONCLUSIONS: The extracts of prop roots of P. fascicularis produce significant analgesic and anti-inflammatory activities, supporting the traditional application of this herb in treating various diseases associated with inflammation and pain.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Edema/tratamento farmacológico , Dor/tratamento farmacológico , Pandanaceae/química , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Ácido Acético/efeitos adversos , Analgésicos/química , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Artrite Reumatoide/tratamento farmacológico , Carragenina/efeitos adversos , Cromatografia , Edema/induzido quimicamente , Etanol/química , Humanos , Indometacina/farmacologia , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Dor/induzido quimicamente , Medição da Dor , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Raízes de Plantas/química , Ratos
19.
Curr Eye Res ; 36(10): 918-29, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21950697

RESUMO

PURPOSE: Dexamethasone (DXN) is an effective anti-inflammatory drug in the treatment of acute and chronic eye disease such as uveitis. It is relatively lipophilic and permeates biological membranes quite easily. However, its low aqueous solubility limits its clinical usefulness. To circumvent this problem Hydroxypropyl-ß-cyclodextrin (HP-ß-CD) was used as solubilizer and penetration enhancer for DXN. The purpose of this study was to develop HP-ß-CD based pH-induced mucoadhesive hydrogel for ophthalmic delivery of DXN to treat uveitis. MATERIALS AND METHODS: The formation of inclusion complex of DXN with HP-ß-CD was characterized in solution and solid states by phase solubility, X-ray diffractometry and IR spectrum analyses. To improve ocular retention and sustained action Carbopol 980 NF and sodium carboxymethylcellulose (NaCMC) were added to the formulations as phase transition and mucoadhesive agents, respectively. RESULTS: The HP-ß-CD-based hydrogel system enhanced the solubility of DXN and the apparent stability constant (k') of the DXN-HP-ß-CD inclusion complex was found to be 258.62 M(-1). The optimum concentrations of Carbopol 980NF and NaCMC for the mucoadhesive hydrogel were 0.2% (w/v) and 0.4% (w/v), respectively. This mucoadhesive hydrogel could flow freely under non-physiological condition and showed the character of pseudoplastic fluid under both physiological and non-physiological conditions. In vitro release of DXN from the HP-ß-CD complex in simulated tear fluid (STF, pH- 7.4), was influenced significantly by the properties and concentration of Carbopol and NaCMC. In vivo studies in rabbit eye showed a marked improvement in anti-inflammatory activity of mucoadhesive hydrogel-treated eye compared with a marketed solution formulation in a uveitis-induced rabbit eye model. CONCLUSION: The developed HP-ß-CD-based mucoadhesive system is a viable alternative to conventional eye drops of DXN due to its ability to enhance bioavailability through its longer precorneal residence time and ability to sustain the release of the drug.


Assuntos
Anti-Inflamatórios/farmacocinética , Dexametasona/farmacocinética , Excipientes/farmacologia , beta-Ciclodextrinas/farmacologia , 2-Hidroxipropil-beta-Ciclodextrina , Resinas Acrílicas/química , Animais , Humor Aquoso/metabolismo , Disponibilidade Biológica , Carboximetilcelulose Sódica/química , Contagem de Células , Modelos Animais de Doenças , Sistemas de Liberação de Medicamentos , Hidrogéis , Concentração de Íons de Hidrogênio , Soluções Oftálmicas , Coelhos , Espectrofotometria Infravermelho , Uveíte Anterior/metabolismo , Viscosidade , Difração de Raios X
20.
Sci Pharm ; 78(4): 941-57, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-21179327

RESUMO

The objective of this study was to formulate sodium alginate based ophthalmic mucoadhesive system of gatifloxacin and its in vitro antibacterial potential on pathogenic microorganisms, Staphylococcus aureus and Escherichia coli. Sodium carboxymethylcellulose (NaCMC) was added to the formulations to enhance the gel bioadhesion properties. The prepared formulations were evaluated for their in vitro drug release, gelation behaviour, rheological behavior, and mucoadhesion force. All formulations in non-physiological and physiological condition showed pseudo plastic behavior. Increase in the concentration of sodium alginate and sodium CMC enhanced the mucoadhesive force significantly. In vitro release of gatifloxacin from the system in simulated tear fluid (STF, pH â 7.4), was influenced significantly by the properties and concentration of sodium alginate, NaCMC. Significant reduction in total bacterial count was observed between control and treatment groups with both the test organisms.

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