DEVELOPMENT OFRIZATRIPTAN BENZOATE MICROSPHERES FOR NOSE TO BRAIN TARGETING

Objective: Oral administration of rizatriptan benzoate shows poor bioavailability due to first pass metabolism, which can be avoided by nasal administration of drugs. Additionally, the nasal administration provides faster onset of action, which is desired to get relief from the intense pain of a migraine. The present research work was emphasised on design, development and evaluation of mucoadhesive microspheres for nasal delivery of rizatriptan benzoate through a systematic approach. Methods: The microspheres of rizatriptan benzoate were prepared by the w/o/w double emulsion solvent diffusion method using the non-aqueous medium. Critical formulation and process parameters were identified through preliminary trial batches and 2[4-1] fractional factorial design was employed using polymer concentration (X1:2-5%), drug to polymer ratio (X2:1:2-1:6), amount of liquid paraffin (X3:100-200 ml) and the amount of magnesium stearate (X4:100-150 mg) as independent variables. Results: Design batches were evaluated for percent yield (50-78%), percent entrapment efficiency (62-85%), drug loading (7.5-30%), % mucoadhesion (47-75%) and drug release at 6 h (44-78%). Scanning electron microscopic (SEM) study showed that microspheres were of 50 µm in size and spherical in shape with a smooth surface. The optimised batch (D10) showed 85% entrapment efficiency and 66.6% drug release within 6 h. The developed microspheres could be used to deliver rizatriptan benzoate through nasal administration for treatment of a migraine. Conclusion: The developed microspheres can be considered as a promising system for nasal delivery system of rizatriptan benzoat

Computational nanoscience and technology

Nanoscience and nanotechnology are the most widely utilized field of science in human healthcare, tissue engineering, food and agriculture. It has several advantages, such as superior surface area and nano-sized molecular structure. Nanomaterial properties like elasticity, mechanical characteristics like hardness, tensile strength, and magnetic and optical properties. It has capability to store high energy, which makes them applicable in the healthcare system. “Executable biology” is applied to the computational model of physiological processes. These models have the advantage of computer science and simulation of pharmacokinetic study. Because of their high potential and computational power, they are widely accepted in pharmaceutical research. US-FDA has tested and utilized computational models in manufacturing various pharmaceutical equipment's that also can be used in drug discovery and manufacturing. These models can create exact validated in vitro and in vivo pharmacological systems, which helps to obtain faster, accurate and more pertinent human data. These models suffer from simplicity, versatility and lack of cumulative research. Multiscale simulations, like the ones based on coarse-graining, are important areas for future research. More significantly, a collaboration between the pharmaceutical industry and computational scientists involved in this field could assist in work in areas wherein molecular dynamic simulations can influence substantially. In this review, different drug target identification models via chemo genomic methods are explained, and the advantages of computational modeling over mathematical model is studied. It also focuses on a wide range of simulation techniques, biomedical applications and challenges of computational modelling. Finally, it gives a brief account of compounds studied using computational modeling and its future perspectives

Nanofibers: A current era in drug delivery system

Nanofibers have a large area of surface variable 3D topography, porosity, and adaptable surface functions. Several researchers are researching nanofiber technology as a potential solution to the current problems in several fields. It manages cardiovascular disorders, infectious diseases, gastrointestinal tract-associated diseases, neurodegenerative diseases, pain treatment, contraception, and wound healing. The nanofibers are fabricated using various fabrication techniques, such as electrospinning, phase separation, physical Fabrication, and chemical fabrication. Depending on their intended use, nanofibers are manufactured using a variety of polymers. It comprises natural polymers, semi-synthetic polymers, synthetic polymers, metals, metal oxides, ceramics, carbon, nonporous materials, mesoporous materials, hollow structures, core-shell structures, biocomponents, and multi-component materials. Nanofiber composites are a good alternative for targeted gene delivery, protein and peptide delivery, and growth factor delivery. Thus, nanofibers have huge potential in drug delivery, which enables them to be used for various applications and can revolutionize these therapeutic areas. This review systematically studied nanofibers' history, advantages, disadvantages, types, and polymers used in nanofiber technology. Further, polymers and their types used in the preparation of nanofibers were summarised. Mainly review article focuses on the fabrication method, i.e., electrospinning and its types. Finally, the article discussed the applications and recent advancements of nanofabrication technology

Levonorgestrel Microneedle Array Patch for Sustained Release Contraception: Formulation, Optimization and In Vivo Characterization

Background: The goal of this work was to develop a levonorgestrel liposome-loaded microneedle array patch for contraception. Methods: Levonorgestrel-loaded liposome was formulated by a solvent injection technique, characterized, and studied. Results: The formulated liposomes were characterized for particle size (147 ± 8 nm), polydispersity index (0.207 ± 0.03), zeta potential (−23 ± 4.25 mV), drug loading (18 ± 3.22%) and entrapment efficiency (85 ± 4.34%). A cryo high-resolution transmission electron microscopy and cryo field emission gun scanning electron microscopy study showed spherical shaped particles with a smooth surface. The in vitro drug release and in vivo pharmacokinetic study showed sustained behaviour of Levonorgestrel for 28 days. Conclusion: The levonorgestrel liposome-loaded microneedle array patch showed better contraception than the drug-loaded microneedle array patch

PHARMACOLOGICAL EVALUATION OF MARKETED POLYHERBAL FORMULATION

Introduction: - Rheumatoid arthritis (RA) is a chronic systemic inflammatory disorder that may affect many tissues and organs – skin, blood vessels, heart, lungs and muscles. But principally attacks the joints, producing a non-supportive proliferative sinusitis that often progresses to destruction of the articular cartilage and ankylosis of the joints. Rhumapar tablet is a marketed polyherbal formulation believed to have the potential for providing relief to rheumatoid arthritis (RA) patients.Objective: - Investigations have been carried out using rats as experimental models, to assess the anti inflammatory and anti arthritic potential of Rhumapar tablet. In-vitro anti-oxidant study has been carried out using different in-vitro models.Result:- The results obtained demonstrate that Rhumapar tablet can significantly and dose-dependently inhibit carrageenan-induced rat paw oedema (the inhibition at 3 hour was greater than at 1 hour after induction of oedema).Tablet can also significantly inhibit granuloma formation in cotton pellet induced granuloma model. It also showed significant anti-arthritic activity in Freund's complete adjuvant (FCA) induced arthritis. The responses were statistically significant when they were compared with the control.Conclusion: - It has been indicated that formulation possesses anti- inflammatory and anti-arthritic activities that are probably mediated through inhibition of prostanoid synthesis and free radical scavenging effect.Keywords: Rhumapar tablet, Rheumatoid arthritis, Anti-inflammatory activity, Anti-arthritic activity, Anti-oxidant activity