Formulation and evaluation of baclofen liposome vesicles using lecithin / Formulación y evaluación de vesículas de liposomas de baclofeno usando lecitina

INTRODUCTION: The main aim of present study was to prepare and characterize liposomal formulation of baclofen to improve the effectiveness of the topically applied formulation. METHOD: For the preparation of liposomes, different ratio of lecithin, cholesterol and ethanol were taken but ratio of drug and stearic acid were kept constant and prepared by ethanol injection method. Liposomes were characterized for vesicle size, vesicle shape, entrapment efficiency, in vitro studies, stability studies and in vivo studies. RESULTS: The average particle size of formulated liposome was in the range of 3.98 ± 0.45-4.24 ± 0.65 mim and small unilamellar vesicles with spherical in shape observed. Entrapment efficiency of optimized formulation was 58.67 ± 0.81 %. The maximum % cumulative drug release behaviours were 67.66 ± 5.32 % after 10 h. formulation stored in 4 ± 2 °C temperature shows better stability (64.19 ± 0.26) compared to elevated temperature. Swiss albino mice were used for the in vivo study and exhibit muscle relaxant activity in terms of no. of falls from rota rod apparatus (p value = 0.001). CONCLUSIONS: Baclofen loaded liposomal formulation have shown skeletal muscle relaxant activity in mice suggesting delivery of baclofen from liposomes in the therapeutic range

INTRODUCTION: the use of specific rules to correctly identify ingredients used in cosmetics was essential for their control. This paper analyses the complex process to adapt the INCI terminology between the 1960s and the 1990s. METHOD: analysis of the legislation published in Spain on the control of cosmetic products between the 1940s and the 1990s, focusing on cosmetic's registers and terminologies and nomenclatures used to identify their ingredients. Printed Primary sources, and periodical press have also been consulted. Primary sources have been discussed and contextualized with the help of more recent history of science publications. Results and CONCLUSIONS: The adoption of precise cosmetic nomenclature or terminology was required by health authorities registering these products, as well as for the labelling to inform consumer. The sanitary regulation of cosmetic products was very lax until the development of this industry and its market in Spain in the 1960s. The consolidation of the dermopharmaceutical sector occurred in the 1970s, in part due to the efforts of various pharmaceutical sectors. The gradual introduction of international cosmetic nomenclatures culminated in the 1990s with the official introduction of the INCI terminology in Spain

Development and evaluation of isoniazid loaded silk fibroin microsphere / Desarrollo y evaluación de microesfera de seda Fibroin cargado de isoniacida

Aim: Current experimental investigation is dedicated to prepare microspheres with small size and good sphericity by Phase Separation method using Isoniazid (INH) as model drug. Silk fibroin has unique intrinsic qualities like biodegradability, biocompatibility or release properties and their tunable drug loading capacity. The delivery loading proficiency of the drug molecules in silk spheres be contingent on their charge, and hydrophobicity or subsequent in altered drug release profiles. Methods: In the present work Isoniazid loaded silk fibroin microsphere was prepared by using phase separation method. Microsphere was evaluated for Ultraviolet-visible spectroscopy, Fourier Transform infrared spectroscopy, Entrapment efficiency, Scanning electron microscopy Studies. Results: Scanning electron microscopy studies revealed that Isoniazid Loaded Silk Fibroin Microspheres were spherical. Entrapment Efficiency of Isoniazid loaded Microspheres of different Formulation from F1 to F5 was in range of 53 to 68 %. F3 showed 68.47 % entrapment Efficiency and the optimized formulation drug release was 93.56 % at 24 hours. Conclusion: Experimental report disclosed a new aqueous based formulation method for silk spheres with controllable shape or size and sphere. Isoniazid loaded silk microspheres may act as ideal nano formulation with elaborated studies

Objetivo: La investigación experimental en curso está dedicada a la preparación de microesferas de pequeño tamaño y buena esfericidad mediante el método de separación de fases con isoniazida (INH) como fármaco modélo. La fibroina de seda tiene cualidades intrínsecas únicas como la biodegradabilidad, biocompatibilidad o propiedades de liberación y su capacidad de carga de fármacos ajustable. La aptitud de entrega de carga de las moléculas de fármaco en las esferas de seda estar supeditada a su carga, y la hidrofobicidad o subsiguiente alteración en los perfiles de liberación de fármacos. Métodos: En el presente trabajo la microesfera de fibroina de seda cargada de isoniazida fue preparada utilizando el método de separación de fases. La microesfera fue evaluada por espectroscopia ultravioleta-visible, espectroscopia infrarroja con transformado de Fourier, se midió la eficiencia de atrapamiento y se estudios mediante microscopia electrónica de barrido. Resultados: Estudios con el microscopio de escaneo de electrones revelaron que las microesferas de fibroina cargada de isoniazida eran esféricas. La eficacia de atrapamiento de las microesferas de formulación diferente de F1 a F5 estuvo en el rango de 53 a 68 %. F3 mostró un 68,47 % de eficiencia de atrapamiento y tras optimizar la formulación de liberación de fármacos fue de 93,56 %, a las 24 horas

An Alternative Approach for Acetylation of Amine Terminated Polyamidoamine (PAMAM) Dendrimer / Un enfoque alternativo para la acetilación de la amina terminal del dendrímero de poliamidoamina (PAMAM)

Aim. Polyamidoamine (PAMAM) dendrimers inherent properties have made it the nanocarrier of choice in the current era of innovation. Dendrimer based products are growing and mushrooming like anything in the current time. Although it suffer from hemolytic toxicity which could be reduced by protecting free amino group. Methods. In the present work alternate acetylated method for PAMAM dendrimers was discussed. 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide Linker was used for acetylation. The acetylated conjugate was evaluated for color reaction, Ultraviolet–visible spectroscopy, Fourier Transform infrared spectroscopy, Differential scanning calorimetric, Nuclear magnetic resonance spectra studies. Results. The PAMAM dendrimers were synthesized using divergent approach and further acetylated. Change in λmax values from 282.0 to 282.5 nm was observed for acetylated dendrimers. Characteristic peak of N-H stretch of primary amine at 3284.16 cm-1 was disappeared due to conversion of primary amine to secondary amine. A new peak of -(CO)-NH stretch was obtained at 1640.28 cm-1 (medium) which shows attachment of acetic acid surface group. The changes in Endothermic peak from 120.56 to 110.400C were observed which shows the PAMAM dendrimers surface modifications The peak of –NH2 at 2.99 ppm was replaced by (–NHCOCH3) at 2.42 ppm further supports the proof of acetylation. Conclusions. The spectral data clearly revealed that this approach for acetylation gives considerable amount of acetylation in less time duration with elimination of organic solvent. This method could be employed for regular acetylation of amine terminated nanocarriers. EDC linker mediated capping of amine groups opened a new avenue for acetylation of amine terminated protein/peptides

Objetivos. Las propiedades inherentes de la poliamidoamina (PAMAM) la han convertido en el nanotransportador de elección en la era actual de la innovación. A pesar de que sufren de toxicidad hemolítica que podría ser reducido mediante la protección del grupo amino libre. En el presente trabajo se discutió el método alternativo de acetilación para los dendrímeros PAMAM. Material y Métodos. El enlazador 1-Etill-3-(3-dimetilaminopropil) carbodiimida (EDC) se utilizó para la acetilación. El conjugado acetilado se evaluó mediante la reacción de color, mediante espectroscopia Ultravioleta visible, espectroscopia infrarroja con transformado de Fourrier, Calorimetría Diferencial de barrido y los estudios de los espectros de Resonancia magnetica nuclear. Resultados. Los dendrímeros PAMAM se sintetizaron utilizando el método divergente y más acetilado. Cambio en los valores λmax 282,0 a 282,5 nm se observó para dendrímeros acetilados. El pico característico del NH de amina primaria a 3284,16 cm-1, desapareció debido a la conversión de amina primaria a amina secundaria. Un nuevo pico de - (CO) -NH se obtuvo a 1640,28 cm-1 (medianas), que muestra la unión de grupo de superficie de ácido acético. Se observaron los cambios en el pico endotérmico de 120,56 a 110.40 ºC que muestra las modificaciones superficiales de dendrímeros PAMAM. El pico de -NH2 en 2,99 ppm fue sustituido por (-NHCOCH3) a 2,42 ppm apoya aun más la prueba de acetilación. Conclusión. Los datos espectrales revelaron claramente que este enfoque para la acetilación da considerable cantidad de acetilación en menos tiempo de duración con la eliminación de disolvente orgánico. Este método podría ser empleado para regular la acetilación de las aminas terminales de nanovehículos. El enlazador EDC de grupos amino abre una nueva vía para la acetilación de amina terminales de proteínas / péptidos