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

Self-micro emulsifying drug delivery systems: a strategy to improve oral bioavailability / Sistema de administración de fármacos autoemulsionante: una estrategia para mejorar la biodisponibilidad oral

Aim: Oral route has always been the favorite route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility, thereby pose problems in their formulation. For the therapeutic delivery of lipophilic active moieties (BCS class II drugs), lipid based formulations are inviting increasing attention. Methods: To that aim, from the web sites of PubMed, HCAplus, Thomson, and Registry were used as the main sources to perform the search for the most significant research articles published on the subject. The information was then carefully analyzed, highlighting the most important results in the formulation and development of self-micro emulsifying drug delivery systems as well as its therapeutic activity. Results: Self-emulsifying drug delivery system (SMEDDS) has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the unreceptive environment in gut. Conclusions: This article gives a complete overview of SMEDDS as a promising approach to effectively deal with the problem of poorly soluble molecules

Objetivo: La vía oral siempre ha sido la ruta preferida de administración de fármacos en muchas enfermedades y hasta hoy es la primera forma investigada en el desarrollo de nuevas formas de dosificación. El principal problema en las formulaciones de fármacos orales es la baja y errática biodisponibilidad, lo que resulta fundamentalmente por la escasa solubilidad en agua, con lo que plantean problemas en su formulación. Para la administración terapéutica de los grupos activos lipófilos (BCS clase II drogas), las formulaciones a base de lípidos están teniendo cada vez más atención. Métodos: Con ese objetivo, a partir de los sitios web de PubMed, HCAplus, Thomson, y sus registros se utilizaron como fuentes principales para llevar a cabo la búsqueda de los artículos de investigación más importantes publicados sobre el tema. A continuación, la información fue analizada cuidadosamente, poniendo de relieve los resultados más importantes en la formulación y desarrollo de sistemas de administración de fármacos auto-emulsionante micro, así como su actividad terapéutica. Resultados: El sistema de administración de fármacos autoemulsionante (SMEDDS) ha ganado más atención debido a la mejorada que permite la reducción de la biodisponibilidad oral en dosis, los perfiles temporales más consistentes de la absorción del fármaco, la orientación selectiva de fármaco (s) hacia la ventana de absorción específica en el tracto gastrointestinal, y la protección del fármaco (s) desde el entorno poco receptivo en el intestino. Conclusiones: Este artículo proporciona una visión completa de SMEDDS como un enfoque prometedor para abordar eficazmente el problema de moléculas poco solubles

Medicinal Effect of Nutraceutical Fruits for the Cognition and Brain Health.

The recent era is witnessing evaluation of medicinal and nutritional value of fruits and fruit juices for the management and prevention of brain diseases like headache stress, anxiety, hypertension, and Alzheimer's and Parkinson's diseases by the scientists and researchers worldwide. Fruits possess various chemicals such as antioxidants and polyphenols, which reduce and balance the effect of hormone in brain responsible for brain disease. Natural remedy is cheap, easily available, nontoxic, and easy to prepare and provides good mental health as compared to other remedies. The main objective of this review is to acknowledge medicinal benefits of fruits for the cognition and management of brain disease.

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

Protein and Peptide in Drug Targeting and its Therapeutic Approach / Las proteínas y péptidos en la orientación de fármacos y su abordaje terapéutico

Aim. The main aim of this review article is to provide information like advantages of protein and peptides via different routes of drug administration, targeted to a particular site and its implication in drug delivery system. Methods. To that aim, from the web sites of PubMed, HCAplus, Thomson, and Registry were used as the main sources to perform the search for the most significant research articles published on the subject. The information was then carefully analyzed, highlighting the most important results in the development of protein and peptide drug targeting as well as its therapeutic activity. Results. In recent years many researchers use protein and peptide as a target site of drug by a different delivery system. Proteins and peptides are used as specific and effective therapeutic agents, due to instability and side effects their use is complicated. Protein kinases are important regulators of most, if not all, biological processes. Abnormal activity of proteins and peptides has been implicated in many human diseases, such as diabetes, cancer and neurodegenerative disorders. Conclusions. It is concluded that the protein and peptide were used in drug targeting to specific site and also used in different diseased states like cancer, diabetes, immunomodulating, neurodegenerative effects and antimicrobial activity

Objetivo. El objetivo principal de este artículo de revisión es proporcionar información sobre las ventajas de las proteínas y péptidos a través de diferentes vías de administración de fármacos, dirigidos a un sitio en particular y su implicación en el sistema de administración de fármacos. Métodos. Con ese objetivo, los sitios web de PubMed, HCAplus, Thomson, se utilizaron como las principales fuentes para realizar la búsqueda de los artículos de investigación más importantes publicados sobre el tema. La información fue luego cuidadosamente analizada, destacando los resultados más importantes en el desarrollo de proteína y péptido de direccionamiento de drogas, así como su actividad terapéutica. Resultados. En los últimos años muchos investigadores utilizan las proteínas y los péptidos como un sitio diana de fármaco por un sistema de administración diferente. Las proteínas y los péptidos se utilizan como agentes terapéuticos específicos y eficaces, debido a la inestabilidad y los efectos secundarios de su uso es complicado. Las proteínas quinasas son reguladores importantes de la mayoría, si no todos, los procesos biológicos. La actividad anormal de proteínas y péptidos se ha implicado en muchas enfermedades humanas, tales como diabetes, cáncer y trastornos neurodegenerativos. Conclusión. Finalmente concluyó que la proteína y el péptido se utilizaron en fármaco que se dirige al sitio específico y también se utiliza en diferentes estados de enfermedad como el cáncer, la diabetes, como sustancias inmunomoduladora, efectos neurodegenerativos y actividad antimicrobiana