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1.
Recent Pat Nanotechnol ; 16(2): 139-159, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33781196

RESUMO

AIM: The present study was aimed to developed and optimize the self-nano emulsifying drug delivery system of α-pinene (ALP-SNEDDS) and evaluate its in-vivo anti-Parkinson's activity. BACKGROUND: Different lipid-based drug delivery technologies have been researched to upgrade drug bioavailability and expand their clinical adequacy upon oral administration. Self-emulsifying drug delivery systems (SEDDS) have pulled in developing the interest specifically for self nano emulsifying drug delivery systems (SNEDDS). OBJECTIVE: The present work was attempted to improve the bioavailability of the ALP by defining the role of self-nano emulsifying formulations for its neuroprotective effect. METHODS: Miscibility of the ALP was estimated in various excipient components to select the optimized combination. Self-nano emulsification, thermodynamic stability, the effect of dilution on robustness, optical clarity, viscosity, and conductivity tests were performed. The in-vivo anti-Parkinson's activity of the ALP-SNEDDS formulations were done using Pilocarpine antagonism induced Parkinsonism in rodents. Behavioral tests like tremulous jaw movements, body temperature, salivation, and lacrimation are performed. RESULTS: Two optimized formulations, composed of Anise oil, Tween 80, and Transcutol-HP of Oil: Smix ratio (4:6 and 3:7) were selected. The Smix ratio for both the formulation was 2:1. The particle size was found to consistent with the increase in dilution. The mean negative zeta potential of the formulations was found to be increased with an increase in dilution. The TEM images of the formulations revealed spherical shape of the droplet. The in-vitro drug release profile was found to be significant as compared to plain ALP suspension. CONCLUSION: The results of in-vivo studies indicate that nanosizing and enhanced solubilization of oral ALP-SNEDDS formulations significantly improved the behavioral activities compared to plain ALP suspension.


Assuntos
Nanopartículas , Tensoativos , Monoterpenos Bicíclicos , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Emulsões , Tamanho da Partícula , Solubilidade
2.
J Biochem Mol Toxicol ; 35(11): e22902, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34464010

RESUMO

Oxidative stress (OS) is involved in the multifaceted pathogenic paradigm of neurodegenerative diseases like Parkinson's disease (PD). Monoterpenes like α-pinene (ALP) is considered to be a therapeutically potent antioxidant agent able to attenuate and scavenge various reactive oxygen species and reactive nitrogen species. The present study aimed to evaluate the in vitro and in vivo neuroprotective effect of α-pinene self-emulsifying nanoformulation (ALP-SENF) for PD. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay was done to evaluate the neurotoxic dose of the ALP-SENF; however, the neuroprotective effect was assessed by 6-hydroxydopamine (6-OHDA) induced neurotoxicity model on SH-SY5Y taking NAC (N-acetyl-l-cysteine) as standard. The in vivo anti-Parkinson's activity of the ALP-SENF was compared with that of the plain ALP suspension by using reserpine antagonism and haloperidol-induced Parkinsonism model in rats. Various behavioral tests and biochemical antioxidant enzymes were estimated. The in vitro results revealed that treatment with ALP-SENF at a concentration of 100 and 200 µM was found to show significant neuronal SH-SY5Y cell viability against 50 µM 6-OHDA. ALP-SENF treated animals have seen significant neurobehavioral improvement. Furthermore, the levels of antioxidative enzymes in biochemical test reveals a marked enhancement in the expression of antioxidant enzymes that significantly attenuated the OS induced neurodegeneration. Due to the mechanisms of their antioxidant action, it was probably due to the scavenging of free radicals and the expression of antioxidant enzymes. It also improved neurobehavioral changes induced by reserpine and haloperidol.


Assuntos
Monoterpenos Bicíclicos/farmacologia , Emulsões , Nanoestruturas , Fármacos Neuroprotetores/farmacologia , Oxidopamina/farmacologia , Monoterpenos Bicíclicos/uso terapêutico , Linhagem Celular Tumoral , Humanos , Fármacos Neuroprotetores/uso terapêutico , Doença de Parkinson/tratamento farmacológico , Reprodutibilidade dos Testes
3.
Acta Pharm ; 61(3): 323-34, 2011 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-21945911

RESUMO

The poorly water soluble antidiabetic drug gliclazide was selected to study the effect of excipients on dissolution rate enhancement. Ordered mixtures of micronized gliclazide with lactose, mannitol, sorbitol, maltitol and sodium chloride were prepared by manual shaking of glass vials containing the drug and excipient(s). Different water soluble excipients, addition of surfactant and superdisintegrant, drug concentration and carrier particle size influenced the dissolution rate of the drug. Dissolution rate studies of the prepared ordered mixtures revealed an increase in drug dissolution with all water soluble excipients. The order of dissolution rate improvement for gliclazide was mannitol > lactose > maltitol > sorbitol > sodium chloride. Composite granules of the particle size range 355-710 µm were superior in increasing the drug dissolution rate from ordered mixtures. Reducing the carrier particle size decreased the dissolution rate of the drug as well as the increase in drug concentration. Kinetic modeling of drug release data fitted best the Hixson-Crowell model, which indicates that all the ordered mixture formulations followed the cube root law fairly well.


Assuntos
Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Gliclazida/química , Hipoglicemiantes/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Portadores de Fármacos/química , Excipientes/química , Gliclazida/uso terapêutico , Humanos , Hipoglicemiantes/uso terapêutico , Lactose/química , Maltose/análogos & derivados , Maltose/química , Modelos Teóricos , Tamanho da Partícula , Farmacocinética , Dodecilsulfato de Sódio/química , Solubilidade , Amido/análogos & derivados , Amido/química , Álcoois Açúcares/química , Tensoativos/química , Suspensões/química , Água
4.
J Microencapsul ; 26(1): 46-53, 2009 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-18608813

RESUMO

The objectives of this investigation were to prepare microspheres of the anti-diabetic drug, metformin hydrochloride, using ethyl cellulose as the polymer and evaluate the encapsulation efficiency and release characteristics in vitro and in vivo; utilizing different microencapsulation techniques. Different proportions of polymer were used to obtain varying drug-polymer ratios. Physical properties, loading efficiency and dissolution rate were dependent on the method chosen for preparation and also on the drug-to-polymer ratio. The addition of surfactant during emulsification and petroleum ether in non-solvent addition process affected release of drug and also size distribution of microspheres. To investigate the type of mechanism that occurs, dissolution data were plotted according to different kinetic models. In vitro release studies show first order and Higuchi model release characteristics being exhibited. All the results were treated statistically to validate the findings. Significant differences in percentage yield, entrapment efficiency and sustaining capacity were seen with microspheres prepared by two different methods. In vivo studies in normal and hyperglycemic mice show faster glucose reduction with microspheres prepared by the evaporation method, whereas the release sustaining effect was more pronounced with microspheres prepared by the non-solvent addition method.


Assuntos
Celulose/análogos & derivados , Preparações de Ação Retardada/química , Composição de Medicamentos/métodos , Metformina/administração & dosagem , Animais , Glicemia/efeitos dos fármacos , Preparações de Ação Retardada/síntese química , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Cinética , Metformina/farmacocinética , Camundongos , Microesferas , Polímeros/síntese química , Polímeros/química
5.
Drug Dev Ind Pharm ; 34(4): 349-54, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18401776

RESUMO

Gastric emptying is a complex process that is highly variable and makes the in vivo performance of drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug delivery systems for more than 12 hours utilizing floating or hydrodynamically controlled drug delivery systems. The objective of this investigation was to develop a floating, depot-forming drug delivery system for an antidiabetic drug based on microparticulate technology to maintain constant plasma drug concentrations over a prolonged period of time for effective control of blood sugar levels. Formulations were optimized using cellulose acetate as the polymer and evaluated in vitro for physicochemical characteristics and drug release in phosphate buffered saline (pH 7.4), and evaluated in vivo in healthy male albino mice. The shape and the surface morphology of the prepared microspheres were characterized by optical microscopy and scanning electron microscopy. In vitro drug release studies were performed and drug release kinetics were calculated using the linear regression method. Effects of stirring rate during preparation and polymer concentration on the size of microspheres and drug release were observed. The prepared microspheres exhibited prolonged drug release (more than 10 hours) and remained buoyant for over 10 hours. Spherical and smooth-surfaced microspheres with encapsulation efficiency ranging from 73% to 98% were obtained. The release rate decreased and the mean particle size increased at higher polymer concentrations. Stirring speed affected the morphology of the microspheres. This investigation revealed that upon administration, the biocompatible depot-forming polymeric microspheres controlled the drug release and plasma sugar levels more efficiently than plain orally given drug. These formulations, with their reduced frequency of administration and better control over drug disposition, may provide an economic benefit to the user compared with products currently available for diabetes control.


Assuntos
Celulose/análogos & derivados , Hipoglicemiantes/farmacocinética , Metformina/farmacocinética , Microesferas , Animais , Glicemia/efeitos dos fármacos , Celulose/química , Química Farmacêutica , Preparações de Ação Retardada , Diabetes Mellitus/tratamento farmacológico , Portadores de Fármacos/química , Trato Gastrointestinal/metabolismo , Modelos Lineares , Masculino , Metformina/administração & dosagem , Camundongos , Microscopia Eletrônica de Varredura , Tamanho da Partícula
6.
Drug Dev Ind Pharm ; 33(10): 1135-41, 2007 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-17963115

RESUMO

The release of poorly water-soluble drug, flurbiprofen, through asymmetric membrane capsule of cellulose acetate containing different pore forming agents like glycerol, polyethylene glycol 400, and dibutyl phthalate, in presence of sodium lauryl sulfate was investigated. The asymmetric membrane was fabricated in the shape of capsule body and cap by phase inversion technique. The type of pore forming agent incorporated had a marked influence on the porosity of the asymmetric membrane. However flurbiprofen due to its poor solubility was unable to create enough osmotic pressure and hence less than 10% of drug was released from all the systems with out SLS. However when the study was conducted with SLS, a maximum release of 72% was observed from the capsule with 70% glycerol. The release rates were found to increase with the increase in the concentration of pore forming agent and the amount of SLS encapsulated.


Assuntos
Sistemas de Liberação de Medicamentos , Flurbiprofeno/administração & dosagem , Cápsulas , Flurbiprofeno/química , Membranas Artificiais , Pressão Osmótica , Permeabilidade , Porosidade
7.
Acta Pharm ; 57(3): 343-50, 2007 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-17878113

RESUMO

An asymmetric membrane capsule of cellulose acetate for osmotic delivery of flurbiprofen has been developed and influence of osmogents and solubilizing agent on in vitro drug release were evaluated. The capsule membrane was prepared by the phase inversion technique. To ensure the osmotic delivery of drug, two approaches were adopted: (i) the drug was encapsulated with osmogents like sodium chloride and mannitol to increase the osmotic pressure of the core, and (ii) the drug was encapsulated with sodium lauryl sulfate in the core of the formulation to increase the solubility and thus its osmotic pressure. Scanning electron microscopy of the membrane confirmed its porous, dense asymmetric nature. Dye test revealed in situ pore formation. The in vitro release study showed that as the proportion of osmogent and solubilizing agent was increased the release rate also increased. A good correlation was observed between the zero-order rate constant and the amount of the osmogent and solubilizing agent used.


Assuntos
Cápsulas/química , Sistemas de Liberação de Medicamentos/métodos , Flurbiprofeno/administração & dosagem , Corante Amaranto/química , Análise de Variância , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Celulose/análogos & derivados , Celulose/química , Difusão , Flurbiprofeno/química , Flurbiprofeno/farmacocinética , Manitol/química , Microscopia Eletrônica de Varredura/métodos , Concentração Osmolar , Osmose , Pressão Osmótica , Porosidade , Cloreto de Sódio/química , Dodecilsulfato de Sódio/química , Solubilidade , Tecnologia Farmacêutica/métodos
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