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1.
AAPS PharmSciTech ; 25(5): 134, 2024 Jun 11.
Artigo em Inglês | MEDLINE | ID: mdl-38862663

RESUMO

Inclusion complexes require higher concentration of Beta cyclodextrins (ßCD) resulting in increased formulation bulk, toxicity, and production costs. This systematic review offers a comprehensive analysis using Quality by design (QbD) as a tool to predict potential applications of Polyvinylpyrrolidone (PVP) as a ternary substance to address issues of inclusion complexes. We reviewed 623 documents from 2013 to 2023 and Eighteen (18) research papers were selected for statistical and meta-analysis using the QbD concept to identify the most critical factors for selecting drugs and effect of PVP on inclusion complexes. The QbD analysis revealed that Molecular weight (MW), Partition coefficient (Log P), and the auxiliary substance ratio directly affected complexation efficiency (CE), thermodynamic stability in terms of Gibbs free energy (ΔG), and percent drug release. However, Stability constant (Ks) remained unaffected by any of these parameters. The results showed that low MW (250), median Log P (6), and a ßCD: PVP ratio of 2:3 would result in higher CE, lower G, and improved drug release. PVP improves drug solubility, enhances delivery and therapeutic outcomes, and counteracts increased drug ionization due to decreased pH. In certain cases, its bulky nature and hydrogen bonding with CD molecules can form non-inclusion complexes. The findings of the study shows that there is potential molecular interaction between PVP and ß-cyclodextrins, which possibly enhances the stability of inclusion complexes for drug with low MW and log P values less than 9. The systematic review shows a comprehensive methodology based on QbD offers a replicable template for future investigations into drug formulation research.


Assuntos
Ciclodextrinas , Povidona , Solubilidade , beta-Ciclodextrinas , beta-Ciclodextrinas/química , Química Farmacêutica/métodos , Ciclodextrinas/química , Liberação Controlada de Fármacos , Excipientes/química , Peso Molecular , Projetos Piloto , Povidona/química , Termodinâmica
2.
Curr Pharm Des ; 29(36): 2853-2866, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37946351

RESUMO

Many methods, including solid dispersion, micellization, and inclusion complexes, have been employed to increase the solubility of potent drugs. Beta-cyclodextrin (ßCD) is a cyclic oligosaccharide consisting of seven glucopyranoside molecules, and is a widely used polymer for formulating soluble inclusion complexes of hydrophobic drugs. The enzymatic activity of Glycosyltransferase or α-amylase converts starch or its derivatives into a mixture of cyclodextrins. The ßCD units are characterized by α -(1-4) glucopyranose bonds. Cyclodextrins possess certain properties that make them very distinctive because of their toroidal or truncated cage-like supramolecular configurations with multiple hydroxyl groups at each end. This allowed them to encapsulate hydrophobic compounds by forming inclusion complexes without losing their solubility in water. Chemical modifications and newer derivatives, such as methylated ßCD, more soluble hydroxyl propyl methyl ßCD, and sodium salts of sulfobutylether-ßCD, known as dexolve® or captisol®, have envisaged the use of CDs in various pharmaceutical, medical, and cosmetic industries. The successful inclusion of drug complexes has demonstrated improved solubility, bioavailability, drug resistance reduction, targeting, and penetration across skin and brain tissues. This review encompasses the current applications of ß-CDs in improving the disease outcomes of antimicrobials and antifungals as well as anticancer and anti-tubercular drugs.


Assuntos
Ciclodextrinas , Humanos , Ciclodextrinas/farmacologia , Ciclodextrinas/química , Solubilidade , Interações Hidrofóbicas e Hidrofílicas , Polímeros
3.
Int J Pharm ; 618: 121605, 2022 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-35227804

RESUMO

Chemopreventive properties of resveratrol has been studied for decades. Despite its potential for chemotherapeutic advancement, the compound has pharmaceutical limitations, such as, the drug has a poor pharmacokinetic profile and low bioavailability. Studies have comforting results that that the nano-formulations may aid the future resveratrol drug development. Resveratrol can also be encapsulated as co-drug with an anticipation of gaining improved targeting and pharmacokinetic parameters, as well as achieving desired therapeutic plasma levels. It has been envisaged that the nanoformulations can also address the issue of drug accumulation, which may lead to hepatotoxicity. Nanoformulations can bring a major improvement in the bioavailability of resveratrol but still the formulation still suffers with pharmacokinetics issues clinically. This review encompasses the pharmacokinetics barriers associated with resveratrol and a possible suggestion to overcome those barriers for improving absorbance, reducing toxicity andimproving the drug releaseand encapsulation efficiency. The article also suggest that co-administration of resveratrol with chemotherapeutic drugsmust be tested in vivo on a wide range of cancers to avoid accidental proliferation exacerbation. The review's focusses on the resveratrol formulation and make suggestions for improvements in order to overcome the pharmacokinetic and toxicity issues.


Assuntos
Neoplasias , Estilbenos , Disponibilidade Biológica , Humanos , Neoplasias/tratamento farmacológico , Preparações Farmacêuticas , Resveratrol/farmacocinética , Estilbenos/farmacocinética
4.
CNS Neurol Disord Drug Targets ; 21(10): 994-1003, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34939554

RESUMO

Epilepsy is known as one of the major challenges for medical science. The sudden appearance of a seizure has been a significant health emergency as it may lead to further complications. Although key advancements have been achieved in terms of pharmacological approaches for epilepsy, many issues remain uncertain. Lipid carriers have been at the forefront, especially in neurodegenerative diseases, such as epilepsy, Alzheimer's, dementia, etc. The blood-brain barrier still appears to be a major impediment in the successful treatment of epileptic seizures. This is mainly due to the limited bioavailability of most anti-convulsant drugs. The present review encompasses the issues underlying the current approach for epilepsy drug treatment and highlights the newer, novel, and more precise drug delivery system to manage seizures. The advantage of using a lipidbased delivery system is its superior absorption in the brain cells. Ample evidence shows that reducing the particle size also infuses the drug easily through the blood-brain barrier. The application of liposomes, polymeric nanoparticles, metallic nanoparticles, and solid lipid nanoparticles for the treatment and management of epilepsy has been highlighted in the present review. This review provides an overview of the current status of the treatment and recent advances in the treatment of epilepsy.


Assuntos
Epilepsia , Nanopartículas , Barreira Hematoencefálica , Sistemas de Liberação de Medicamentos , Epilepsia/tratamento farmacológico , Humanos , Lipossomos/uso terapêutico , Nanopartículas/uso terapêutico , Nanotecnologia , Convulsões/tratamento farmacológico
5.
Braz. J. Pharm. Sci. (Online) ; 58: e18655, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1364423

RESUMO

Abstract Periodontitis is an oral disease associated with inflammation and pain with swollen and bleeding gums. In the present study, dental pastes containing NSAIDs, namely, diclofenac sodium and nimesulide (1 % w/w) were prepared to treat periodontitis. Dental pastes of diclofenac sodium and nimesulide (1 % w/w) were prepared with/without mucoadhesive hydrocolloid polymers such as sodium carboxy methyl cellulose (NaCMC), hydroxyl ethyl cellulose (HEC) and methyl cellulose (MC) by conventional trituration method. The pH, drug content, viscosity, tube spreadability and tube extrudability of these prepared dental pastes were measured. These dental pastes of diclofenac sodium and nimesulide (1 % w/w) were characterized by FTIR analyses for drug-excipient compatibility. The in vitro drug releases from these dental pastes in 6.4 pH phosphate buffer solution displayed sustained release over longer period and the drug release rate was found to be decreased when the concentration of mucoadhesive polymer was increased. These dental pastes displayed good adhesion to the oral mucosa revealing more retention time in mouth when tested for ex vivo mucoadhesion using bovine cheek pouch. The stability study results reveal that the DC3 and NC3 dental paste formulations were found stable enough over a longer period in different storage conditions. The present study revealed that the prepared mucoadhesive dental pastes of diclofenac sodium and nimesulide (1 % w/w) had good adhesion with the oral mucosa to maintain consistent release of drugs over prolonged time.


Assuntos
Cremes Dentais/análise , Preparações Farmacêuticas , Anti-Inflamatórios não Esteroides/análise , Boca , Mucosa Bucal/anormalidades , Periodontite , Técnicas In Vitro/métodos , Diclofenaco/efeitos adversos , Doença/classificação , Espectroscopia de Infravermelho com Transformada de Fourier , Liberação Controlada de Fármacos , Gengiva/anormalidades , Inflamação/complicações
6.
Hum Vaccin Immunother ; 17(3): 785-790, 2021 03 04.
Artigo em Inglês | MEDLINE | ID: mdl-32838636

RESUMO

Malaysia is a predominant Muslim country and the recent surge in vaccine-preventable disease enticed us to conduct a survey to measure the Knowledge, Attitude and Perception of Muslim parents toward vaccination process. The data were collected under four segments such as demography, Knowledge, Attitude and Perception. The questionnaire had high internal consistency (0.823) for Cronbach's alpha. The sociodemographic determinants such as marital status (OR = 1.12; 0.91-1.38;p < .05), education level (college OR = 1.35; 1.12-1.64;p < .05, secondary OR = 1.22; 1.01-1.47;p < .05) and the occupation of parents (OR = 1.25; 1.07-1.45;p < .05) were observed affecting the Knowledge score significantly. Majority of Malaysian Muslim parents believed that "vaccine is not prohibited in Islam" and most of them also rejected the belief that "all vaccines are non halal and hence should be avoided". None of the sociodemographic determinants significantly affected the Attitude and Perception score of the Muslim parents. It was observed that the Attitude and Perception score did not establish any association with any of the socio-demographic determinants and hence the null hypothesis that Malaysian Muslim parents had positive Attitude and good Perception toward vaccination process was accepted.


Assuntos
Conhecimentos, Atitudes e Prática em Saúde , Islamismo , Estudos Transversais , Humanos , Malásia , Pais , Percepção , Inquéritos e Questionários , Vacinação
7.
Curr Pharm Des ; 26(34): 4272-4276, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32693760

RESUMO

Cancer and tumor have been major reasons for numerous deaths in this century across the world. Many strategies have been designed to treat, diagnose, or prevent cancer. The success of chemotherapy largely depends on drug targeting. The advent of nanotechnology has vastly improved drug delivery for targeting and diagnosis. Nevertheless, the accuracy of drug targeting with polymeric nanoparticles has always been questionable. The polymeric nanoparticles synthesized from varieties of lipid-based compounds or combined with vectors, such as liposomes, ethosomes, and transfersomes, may allow the drug to overcome the issue of resistance to drug absorption in biological membranes. The combined effects of lipid-based nanocarriers are known to improve the efficacy and accuracy of polymeric nanoparticles. The present review explores the application of lipid based nanocarriers in the treatment and diagnosis of cancer A special focus is given to the use of lipid-based nanocarriers in the treatment, diagnosis, and mitigation of cancer located in blood, brain, lung, and colon. The treatment of these cancers has always been questionable as the chances of relapse are very high. The review encompasses the use of lipid-based nanocarriers in targeting tissue-specific cancer cells.


Assuntos
Nanopartículas , Neoplasias , Portadores de Fármacos/uso terapêutico , Sistemas de Liberação de Medicamentos , Humanos , Lipídeos/uso terapêutico , Neoplasias/tratamento farmacológico
8.
Hum Vaccin Immunother ; 15(11): 2544-2551, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31070987

RESUMO

Aim: Mothers knowledge and attitude toward childhood vaccination influence uptake is the most adequate tool and preventive aspects to infectious disease epidemics. The present study assesses and measures knowledge and attitude of postnatal mothers toward vaccination.Methods and results: The present study adopted a cross-sectional study design, whereby 200 postnatal mothers were identified during their postnatal visit to clinics. The subjects were accessed using questionnaire to assess the level of knowledge and attitude of mothers regarding vaccination. The objectives were to study the level of knowledge, the attitude, and to find the association between knowledge and attitude of the study subjects. The data were analyzed using SPSS version 16. The results was analyzed through chi-square test. The association between age (p = .031), education (p = .021), occupation (p = .013), and knowledge score toward vaccination was found to be statistically significant. However, ethnicity (p = .127), employment (p = .197), and mode of delivery (p = .750) toward mothers vaccination knowledge were not significant for the study. Mothers education, age, and occupation were found to be associated with attitude toward childhood vaccination. No association was found between ethnicity, employment, and mode of delivery with attitude of childhood vaccination.Conclusion: More than half of the studied mothers had good knowledge scores on vaccination, more than two-thirds of the studied mothers had good attitude scores on vaccination. However, the religious misconception and fear of autism was the main cause of vaccine resistance in Malaysia.


Assuntos
Saúde da Criança , Conhecimentos, Atitudes e Prática em Saúde , Programas de Imunização , Mães/psicologia , Vacinação/psicologia , Adolescente , Adulto , Estudos Transversais , Feminino , Humanos , Malásia , Avaliação das Necessidades , Cuidado Pós-Natal , Inquéritos e Questionários , Adulto Jovem
9.
Hum Vaccin Immunother ; 15(1): 156-162, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30199299

RESUMO

The human papilloma virus (HPV) is known to be a major causative agent of cervical cancers and warts, limited study has been conducted on its associated factors among health care students and professionals in Malaysia. The present study was carried to explore the knowledge, understanding, attitude, perception and views about HPV infection and vaccination. A total of 576 respondents were recruited to complete a self-administered questionnaire through convenience sampling across Malaysia. 80.% and of the females respondents exhibited a positive attitude towards knowledge and understanding and 60% exhibited a positive towards attitude, perception and views. Almost 65% of the population were in agreement that HPV can be transmitted sexually, and 56.7% felt strongly that sexually active persons should essentially be vaccinated. The corresponding values were somewhat lower among the male respondents. Regression analysis suggested that knowledge and understanding were strong associated with gender, age, and occupation. Attitude, perception and views were also evidently associated with gender and age. The Ministry of Health should take steps to improve awareness among the citizens. Efforts should be made to educate people on the risk of HPV as a sexually transmitted diseases associated with HPV, and on the availability of discounted and safe HPV vaccines in government hospitals to increase the uptake rate of HPV vaccines among the Malaysian population.


Assuntos
Conhecimentos, Atitudes e Prática em Saúde , Pessoal de Saúde/psicologia , Infecções por Papillomavirus/prevenção & controle , Estudantes/psicologia , Vacinação/psicologia , Adolescente , Adulto , Estudos Transversais , Feminino , Humanos , Malásia , Masculino , Vacinas contra Papillomavirus/administração & dosagem , Aceitação pelo Paciente de Cuidados de Saúde , Inquéritos e Questionários , Neoplasias do Colo do Útero/prevenção & controle , Adulto Jovem
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