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1.
Recent Pat Biotechnol ; 18(1): 2-21, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38205772

RESUMO

The last few decades have seen a rise in the number of deaths caused by neurological disorders. The blood-brain barrier (BBB), which is very complex and has multiple mechanisms, makes drug delivery to the brain challenging for many scientists. Lipid nanoparticles (LNPs) such as nanoemulsions, solid-lipid nanoparticles, liposomes, and nano lipid carriers (NLCs) exhibit enhanced bioavailability and flexibility among these nanocarriers. NLCs are found to be very effective. In the last few decades, they have been a center of attraction for controlled drug delivery. According to the current global status of specific neurological disorders, out of all LNPs, NLC significantly reduces the cross-permeability of drugs through the BBB due to their peculiar properties. They offer a host of advantages over other carriers because of their biocompatibility, safety, non-toxicity, non-irritating behavior, stability, high encapsulation efficiency, high drug loading, high drug targeting, control of drug release, and ease in manufacturing. The biocompatible lipid matrix is ideally suited as a drug carrier system due to the nano-size range. For certain neurological conditions such as Parkinsonism, Alzheimer's, Epilepsy, Multiple sclerosis, and Brain cancer, we examined recent advances in NLCs to improve brain targeting of bioactive with special attention to formulation aspects and pharmacokinetic characteristics. This article also provides a brief overview of a critical approach for brain targeting, i.e., direct nose-to-brain drug delivery and some recent patents published on NLC".


Assuntos
Portadores de Fármacos , Doenças Neurodegenerativas , Humanos , Encéfalo , Sistemas de Liberação de Medicamentos , Doenças Neurodegenerativas/tratamento farmacológico , Patentes como Assunto
2.
Ther Deliv ; 14(11): 705-720, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-38014488

RESUMO

Aim: To develop a propranolol HCL-loaded liposomal nasal formulation for migraine prophylaxis. Materials & methods: Formulated the liposomes through thin layer hydration method and optimized via design of experiments (DOE). The prepared liposomes were characterized for particle size, zeta potential, PDI, drug entrapment and drug loading. Assessed for in vitro release kinetics, ex vivo permeability, histopathology and stability. Results: Optimized liposomes: 135.52 ± 5.87 nm, -19.9 ± 0.075 mV, 95.41 ± 0.05% entrapment, 43.37 ± 0.02% loading. Showed immediate (30.07 ± 2.09%) and sustained release (95.69 ± 4.58%) over 10 h. Enhanced permeation compared with controls; well-tolerated histopathologically. Conclusion: Liposomal formulation offers promise for intranasal propranolol HCL delivery in migraine prophylaxis, with stability under refrigeration.


Migraines (a type of long-lasting headache) can be helped by a medicine called propranolol HCL. In this study, scientists developed tiny bubbles, called liposomes, which contained propranolol HCL. The liposomes are designed to be inhaled via the nose, where the medicine is released slowly from the liposomes to treat the migraine. In this study, the researchers made the propranolol HCL-containing liposomes and analyzed them in the lab. They found that the liposomes were safe, and can be kept in a cool place for a long time. So, may be able to help treat migraines.


Assuntos
Lipossomos , Transtornos de Enxaqueca , Humanos , Propranolol , Administração Intranasal , Liberação Controlada de Fármacos , Tamanho da Partícula , Sistemas de Liberação de Medicamentos/métodos
3.
Ther Deliv ; 14(5): 337-356, 2023 05.
Artigo em Inglês | MEDLINE | ID: mdl-37403998

RESUMO

Aim: To review the state of the art aspects and contemporary innovative drug delivery strategies, for the treatment of vitreoretinal diseases, their mechanism of action through ocular routes and their future perspectives. Materials & methods: Scientific databases such as PubMed, Science Direct, Google scholar were used to obtain 156 papers for review. The keywords searched were vitreoretinal diseases; ocular barriers; intravitreal injections; nanotechnology; biopharmaceuticals. Results & conclusion: The review explored the various routes which can be used to facilitate drug delivery adopting novel strategies, the pharmacokinetic aspects of novel drug-delivery strategies in treating posterior segment eye diseases and current research. Therefore, this review drives focus into the same and underlines their implications to the healthcare sector in making necessary interventions.


Eye diseases that affect the major part of the eye can create eyesight loss in patients. Even though medicines are now available, there is a need to drive the existing techniques further. These can be done by the use of small sized particles in the treatment, which are easy to reach the site wherever healing is required. Natural medicines and treatment can also benefit people. In this paper, we discuss treatment approaches on these factors and their importance in curing people with eye diseases.


Assuntos
Produtos Biológicos , Oftalmopatias , Humanos , Sistemas de Liberação de Medicamentos/métodos , Oftalmopatias/tratamento farmacológico , Olho , Nanotecnologia
4.
Ther Deliv ; 14(3): 227-249, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-37291865

RESUMO

Periodontitis is a microbiological condition that affects the tissues supporting the teeth. The fundamental to effective periodontal therapy is choosing the suitable antimicrobial and anti-inflammatory agent, together with the proper route of drug administration and delivery system. Intra-periodontal pocket approach with nano drug-delivery systems (NDDS) such as polymeric nanoparticles, gold nanoparticles, silica nanoparticles, magnetic nanoparticles, liposomes, polymersomes, exosomes, nano micelles, niosome, solid lipid nanoparticles, nano lipid carriers, nanocomposites, nanogels, nanofibers, scaffolds, dendrimers, quantum dots, etc., will be appropriate route of drug administration and delivery system. This NDDS delivers the drugs at the site of infection to inhibit growth and promote tissue regeneration. The present review focused on providing comprehensive information on the NDDS for periodontitis, which enhanced therapeutic outcomes via intra-periodontal pocket delivery.


Periodontitis is a problem that can make your teeth fall out. It happens when the tissues that hold your teeth start to break down. Scientists have found a way to help treat it by using tiny things called 'nano drug-delivery systems' or NDDS. These NDDS carry medicine to the infected area and stop the germs from growing. They can also help the tissue around your teeth to heal. Some examples of NDDS are liposomes, polymersomes, exosomes, nanomicelles, and more. Regular treatment with antibiotics may not work as well as NDDS. Using NDDS can make a big difference in how well your teeth and gums heal. In the future, scientists hope to use NDDS to prevent the problem from coming back. This new way of treating periodontitis could be a big help for people with this problem.


Assuntos
Nanopartículas Metálicas , Periodontite , Humanos , Bolsa Periodontal/tratamento farmacológico , Bolsa Periodontal/microbiologia , Ouro , Sistemas de Liberação de Medicamentos , Periodontite/tratamento farmacológico , Periodontite/microbiologia
5.
Pharmaceutics ; 13(10)2021 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-34683933

RESUMO

An acute epileptic seizure is a seizure emergency fatal condition that requires immediate medical attention. IV phenytoin sodium remains the second line therapeutic agent for the immediate treatment of status epilepticus. Phenytoin sodium formulated as nanolipid carriers (NLCs) seems to be promising as an intranasal delivery system for controlling acute seizures. Three different nanosized phenytoin sodium loaded NLCs (<50 nm, 50-100 nm and >100 nm) were prepared by melt emulsification and was further characterised. In vitro drug release studies showed immediate drug release from phenytoin sodium loaded NLCs of <50 nm size, which is highly essential for acute seizure control. The ex vivo permeation study indicated greater permeation from <50 nm sized NLC through the olfactory epithelium compared to thecontrol drug solution. Invivo pharmacokinetic studies revealed higher drug concentration in CSF/brain within 5 min upon intranasal administration of <50 nm sized phenytoin sodium NLCs than the control drug solution and marketed IV phenytoin sodium, indicating direct and rapid nose to brain drug transport through the olfactory epithelium. The study has shown that formulation strategies can enhance olfactory uptake, and phenytoin sodium NLCs of desired particle sizes (<50 nm) offer promising potential for nose to brain direct delivery of phenytoin sodium in treating acute epileptic seizures.

6.
Int J Biol Macromol ; 110: 308-317, 2018 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-29341922

RESUMO

In the present investigation, the effect of timolol maleate loaded ocuserts was studied as an alternative for conventional anti-glaucoma formulation. Ocuserts were prepared using natural polymer sodium alginate and ethyl cellulose. Physico-chemical properties along with drug entrapment efficiency (94-98%), content uniformity (93.1% ±â€¯0.264-98.00% ±â€¯0.321), in vitro drug release (83.42% ±â€¯0.35 at end of 12 h), ex vivo permeation all showed satisfactory results, which was found to follow zero order kinetics. Ex vivo permeation studies showed better results, revealed that the permeability coefficient was dependent on polymer type. The sterility test accelerated stability studies and in vivo studies such as eye irritancy test, in vivo drug release of the optimized ocusert was determined. The anti-glaucoma activity was measured using Schiotz tonometer at different time interval. Significant reduction in Intra ocular pressure (IOP) within 3 days was observed in case of rabbits treated with ocusert in comparison to the rabbit treated with marketed eye drop formulation. Hence timolol maleate loaded ocuserts proved to be a promising and viable alternative over conventional eye formulation for the sustained and controlled ophthalmic drug delivery, targeting the drug within the ocular globe thus improving patient compliance for the treatment of glaucoma.


Assuntos
Glaucoma , Pressão Intraocular/efeitos dos fármacos , Pilocarpina , Timolol , Animais , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacocinética , Preparações de Ação Retardada/farmacologia , Glaucoma/tratamento farmacológico , Glaucoma/metabolismo , Glaucoma/patologia , Cabras , Pilocarpina/química , Pilocarpina/farmacocinética , Pilocarpina/farmacologia , Coelhos , Timolol/química , Timolol/farmacocinética , Timolol/farmacologia
7.
Open Med Chem J ; 11: 222-244, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29399211

RESUMO

BACKGROUND: A novel drug delivery system for treating acute epileptic condition. OBJECTIVE: To develop an intranasal mucoadhesive formulation of Lamotrigine (LTG) loaded insitu gel, for the treatment of epilepsy to avoid possible side effects and first pass metabolism associated with conventional treatment. METHODS: Lamotrigine was loaded into different polymeric solutions of gellan and xanthan gum. RESULTS: All formulations subjected to various evaluation studies were within their acceptable limits. The pH of formulation ranges between 5.8 ±.001 to 6.8 ±.005 indicating that no mucosal irritation is expected as pH was in acceptable range. Invitro drug release from the mucoadhesive insitu gel formulations showed immediate drug release pattern with a maximum drug release of 97.02 ±0.54% for optimized G5 formulation within 20min. Exvivo permeation studies of optimized formulation G5 and control formulation was estimated. Exvivo permeation studies of G5 insitu formulation done for a period of 12 h resulted in slow, sustained release and greater permeability significance(P <0.05) through nasal mucosa when compared to control. Histopathological studies showed that G5 formulation was safer for nasal administration without any irritation. The stability studies indicated that gels were stable over 45 days in refrigerated condition (4±2ºC). CONCLUSION: The intranasal insitu gelling system is a promising novel drug delivery system for an antiepileptic drug lamotrigine which could enhance nasal residence time with increased viscosity and mucoadhesive character and provided better release profile of drug for treating acute epileptic conditions.

8.
J Adv Pharm Technol Res ; 3(1): 9-15, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-22470888

RESUMO

Periodontal pockets act as a natural reservoir filled with gingival crevicular fluid for the controlled release delivery of antimicrobials directly. This article reflects the present status of nonsurgical controlled local intrapocket delivery of antimicrobials in the treatment of periodontitis. These sites have specialty in terms of anatomy, permeability, and their ability to retain a delivery system for a desired length of time. A number of antimicrobial products and the composition of the delivery systems, its use, clinical results, and their release are summarized. The goal in using an intrapocket device for the delivery of an antimicrobial agent is the achievement and maintenance of therapeutic drug concentration for the desired period of time. Novel controlled drug delivery system are capable of improving patient compliance as well as therapeutic efficacy with precise control of the rate by which a particular drug dosage is released from a delivery system without the need for frequent administration. These are considered superior drug delivery system because of low cost, greater stability, non-toxicity, biocompatibility, non-immunogenicity, and are biodegradable in nature. This review also focus on the importance and ideal features of periodontal pockets as a drug delivery platform for designing a suitable dosage form along with its potential advantage and limitations. The microbes in the periodontal pocket could destroy periodontal tissues, and a complete knowledge of these as well as an ideal treatment strategy could be helpful in treating this disease.

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