RESUMEN
Phospholipid-modified solid lipid microparticles (SLMs) of Phospholipon® 90G and 90H encapsulating the hydrophilic drug, gentamicin were produced and loaded into three polymeric hydrogels of Poloxamer 407 and polyacrylic acids (Carbopols® 971P and 974P). The SLMs were characterized by morphology and particle size, drug encapsulation efficiency, thermal properties, pH, and storage stability, whereas the microgels were evaluated for viscosity, spreadability, pH, drug content, and in vitro antimicrobial drug release against five microorganisms (Klebsiella spp., Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa). Our results generally showed Poloxamer 407 microgels of P90H and P90G as having the most desirable properties in terms of fast antibacterial activity on all tested microorganisms, in vitro diffusion-dependent permeation through rat abdominal skin, spreadability, pH, and viscosity, superior to polyacrylic acids microgels.
Asunto(s)
Geles , Gentamicinas/administración & dosificación , Fosfatidilcolinas/química , Fosfolípidos/química , Piel/efectos de los fármacos , Acrilatos/química , Administración Cutánea , Animales , Antiinfecciosos/administración & dosificación , Portadores de Fármacos/química , Hidrogeles/química , Concentración de Iones de Hidrógeno , Lípidos , Masculino , Pruebas de Sensibilidad Microbiana , Tamaño de la Partícula , Poloxámero/química , Ratas , Ratas Wistar , Reología , ViscosidadRESUMEN
BACKGROUND & OBJECTIVES: With the current snags from the use of Artemisinin - combination therapies (ACTs) in malaria treatment in addition to fear of cross- resistance to unrelated drugs, raising the immunocompetence of individuals in malaria endemic areas by vaccination is the best approach to malaria - free world. METHODS: Water - soluble cationic derivative, N, N, N- trimethylchitosan (TMC) was synthesized from chitosan. Nanoparticles of the TMC were prepared in various media [milliQ water, Na2CO3 (pH 10.92), Na2HPO4 (PBS, pH 9.01 and alhydrogel® ] which were characterized as adjuvants for possible vaccine delivery. The nanoparticles were characterized for particle size, surface charge and morphology using microscopy (Phase contrast microscope and Confocal laser scanning microscope), and Malvern zetasizer Nano - ZS. Time - resolved particle size analysis was performed after one month storage of the TMC nanoparticles at 4°C. RESULTS: The result of the study showed that PBS was the best medium that produced cationic, monodispersed and stable TMC nanoparticles of < nm forming a compatibly homogeneous system even upon storage. Details of the polyelectrolyte - doped nanoparticles in PBS showed clear coatings due to Sodium poly (styrene sulfonate) [PSS, MW ~70 kDa] at the periphery of the particles and a fluorescent core with some tiny central hollow cavities implying that the nanoparticles can either entrap the vaccine candidate into the hollow cavities or adsorb them unto the surface of the peripheral polyelectrolyte coatings. INTERPRETATION & CONCLUSION: This preliminary study established that TMC has the desired qualities for the intending antigen delivery. Further research regarding the biological activity of this TMC is indicated.
Asunto(s)
Quitosano/química , Vacunas contra la Malaria/administración & dosificación , Malaria/prevención & control , Nanopartículas/química , Adyuvantes Inmunológicos/síntesis química , Adyuvantes Inmunológicos/química , Antígenos de Protozoos/administración & dosificación , Antígenos de Protozoos/química , Antígenos de Protozoos/inmunología , Quitosano/síntesis química , Quitosano/inmunología , Portadores de Fármacos , Estabilidad de Medicamentos , Humanos , Espectroscopía de Resonancia Magnética , Malaria/inmunología , Malaria/parasitología , Vacunas contra la Malaria/química , Vacunas contra la Malaria/inmunología , Tamaño de la Partícula , Solubilidad , Propiedades de SuperficieRESUMEN
P90Gylation refers to the modification of lipid molecules by one or more phospholipid chains. Phospholipon 90G (P90G) contains about 94.0% of phosphatidylcholine stabilized with 0.1% ascorbyl palmitate and is a safe (GRAS) FDA-approved parenteral excipient with wide applications in drug delivery. P90Gylated-Softisan 142 conjugate, otherwise referred to as (SRMS142), has numerous advantages: wetting, solubilization, drug stabilization, emulsification, and modified release. Here, we report an evaluation of solid lipid microparticles (SLMs) formulated from SRMS142 systems as an alternative carrier system for oral glibenclamide administration in diabetic rats. The result of our findings showed that SRMS142 generated an imperfect matrix with numerous spaces that accommodated glibenclamide in a concentration-dependent manner up to 60.58%. The blood glucose-lowering effect of the SLMs was higher than that of a commercial sample.
Asunto(s)
Ácido Ascórbico/análogos & derivados , Glucemia/efectos de los fármacos , Diabetes Mellitus Experimental/tratamiento farmacológico , Portadores de Fármacos , Gliburida/administración & dosificación , Hipoglucemiantes/administración & dosificación , Fosfatidilcolinas/química , Administración Oral , Animales , Ácido Ascórbico/química , Rastreo Diferencial de Calorimetría , Química Farmacéutica , Preparaciones de Acción Retardada , Diabetes Mellitus Experimental/sangre , Modelos Animales de Enfermedad , Composición de Medicamentos , Gliburida/química , Hipoglucemiantes/química , Masculino , Tamaño de la Partícula , Ratas , Ratas Wistar , Solubilidad , Tecnología Farmacéutica/métodosRESUMEN
The decimal assay for additivity (DAA) method was used to evaluate the in vitro interaction of glycine (Gly) with penicillin G (Pen G); cloxacillin (Clox) and ampicillin (Amp) against a clinical isolate of Staphylococcus aureus. In the interaction between Pen G/glycine with biological equivalent factor (BEF) 5 mg/62 mg; the decimal combination of 4 parts Pen G and 6 parts glycine showed amtagpmos; wjo;e ptjers sjpwed addotive effect In the interaction between Clox/glycine with BEF 1.26 og/62.5 mg ony 7:3 combination gave a synergistic effect. Others showed antagonism. In Amp/glycine combination with BEF; 1.74 og/62.5 mg; the decimal combinations of 4:6 gave additive effect; 9:1 gave synergistic effect while 7:3 combinaiton gave indifferent effect
Asunto(s)
Glicina , Penicilinas , InvestigaciónRESUMEN
Goat fat and Tween 65 admixtures were used to formulate self-emulsifying tablets containing diclofenac. The tablets were formulated by pour moulding using a plastic mould. The tablets were evaluated using the following parameters: weight uniformity, absolute drug content, and liquefaction time. The dissolution profile of diclofenac from the self-emulsifying tablets was determined in simulated gastric fluid (SGF) without pepsin. Results obtained indicated that diclofenac could be comfortably administered in the form of self-emulsifying tablets using goat fat and Tween 65 admixtures.