CEFPODOXIME PROXETIL FAST DISSOLVING TABLETS: COMPARATIVE STUDY

Objective: In the present investigation, fast dissolving tablets of cefpodoxime proxetil were formulated using superdisintegrants to impart fast disintegration. Methods: In the current study, 12 formulations of fast dissolving tablets of cefpodoxime proxetil were formulated using two different approaches viz., direct compression and sublimation. Three different superdisintegrants viz., croscarmellose sodium, sodium starch glycolate, and crospovidone were used in a different concentration in all the respective formulations. The final powder blend was subjected for the pre-compression evaluation and all the formulations were evaluated for post-compression parameters. Stability studies were also evaluated for the best formulations as per ICH guidelines. Finally, results were statistically analyzed by the application of one way ANOVA test and t-test. Results: Among all the formulations of different approaches, formulation cefpodoxime proxetil 4 (CP4) containing 6% crospovidone as a super disintegrant was showed the best results. In vitro dissolution data revealed that formulation CP4 prepared by direct compression method showed 99.387±0.270% drug release within 15 min whereas the percentage release by formulation prepared by using sublimation showed 83.927±0.735% release. The optimized formulation was further subjected to comparative in vitro study with two marketed formulation of different brands. Conclusion: All the data of all formulations is shows that direct compression approach is the best approach for developing the fast dissolving tablets to enhance the onset of action and bioavailability

Green Synthesis of Silver Atropa Acuminata Nanoparticles: Characterization and Anti-Diabetic Potential

  Background: Atropa acuminata plant, which is also known as the maitbrand or Indian belladonna, belongs to the family Solanaceae and is closely related to the deadly nightshade of Europe and North Africa used in the treatment of various diseases. Objectives: The main objective is to investigate the antidiabetic potential of silver nanoparticles of Atropa acuminata. Methods: In this study green synthesis of silver nanoparticles was carried out. The current study engross the green synthesis of A. acuminata roots by reducing silver ions, where ultraviolet (UV) spectral analysis and transmission electron microscopy confirmed nanoarchitecture. The optimized silver nanoparticles were characterized for shape, size and morphological features by various techniques viz., SEM, TEM EDXA and XRD. The optimized formulation was further subjected for lipid peroxidation assay and in vitro antidiabetic assay in order to understand the antidiabetic potential of formulated silver nanoparticles. Results: The Silver nanoparticles of Atropa acuminata roots was successfully prepared by optimizing different concentration of plant extract at different temperatures and stirring speed. The Resultant optimized nanoparticles showed a particle size around 20 nm and -28 mv zeta potential. Further the characterization of optimized AgNPs was carried out. SEM provides the shape, size, and morphological features, whereas EDXA confirms the compositions and distribution of nanoparticles through spectrum and elemental mapping. XRD diffraction analysis revealed the crystalline structure of nanoparticles. Further, Nanoparticles showed a maximum scavenging potential of 82.633±0.116 for superoxide anion free radicals at 100 µg/mL concentration. Among two anti- diabetic assays, the αamylase assay shows a better result of percent inhibition 63 ± 1.32 at 75 μg/ml concentrations. Lastly, in vitro, drug release study revealed a 101.50% cumulative release from Ag- NPs formulation up to 1 hour, which was better than the standard one. Conclusion: This study explores the novel technology of green synthesis for various biomedical applications

Qualitative and Quantitative estimation of Phytoconstituents and Antimycobacterial property of ethanolic extract of Cassia fistula leaf against H37RV test organism

Cassia fistula belongs to the family Caesalpinaceae commonly known as “Golden shower tree” has been used in different traditional system of medicines for various ailments since ancient times. Cassia fistula grows throughout in Bangladesh and in many other Asian countries such as India, China, Hong Kong, Philippines, Malaysia, Indonesia, and Thailand. Sequential extraction of leaves of Cassia fistula was carried out by using different solvents like petroleum ether, chloroform, ethanol, methanol and water in Soxhlet apparatus. Ethanolic extract was investigated for qualitative and quantitative phytochemical studies. Ethanolic extract was also analysed for its antimycobacterial property. Results of the study showed highest yield of the leaf extract in ethanol. Phytochemical studies revealed the presence of secondary metabolites like carbohydrate, proteins, amino acids, steroids, saponins, alkaloids, tannins, phenols and flavanoids. Ethanolic leaf extract showed good inhibitory activity against H37RV test organism. The minimum inhibitory concentration was found to be 2.5μg/ml. Furthermore, the ethanol extract was subjected to LCMS, TLC and HPTLC fingerprinting. Results of LCMS, TLC and HPTLC showed the presence of alkaloids, flavonoids and phenols

PREPARATION AND EVALUATION OF COPPER NANOPARTICLES LOADED HYDROGEL FOR BURNS

Objective: The present study focuses on the development and optimization of copper nanoparticles (CNPs) loaded hydrogel for the treatment of dermal burn injuries. Methods: CNPs gel was prepared by dispersing the variable concentration of polyvinylpyrrolidone (PVP K30) and hydroxypropyl methylcellulose (HPMC) in distilled water, PEG 400, and copper nanoparticles. factor screening study was performed for identification of influential factors, followed by optimization study using three-factor Box-Behnken design. Results: Optimized nanogel formulation, when compared to normal control (NC), shows a significant reduction of pro-inflammatory cytokines (IL-6 = 39.74 % and TNF-α =49.37%) and increased level of anti-inflammatory cytokines (IL-10 = 30.90%), indicating reduced inflammation. Further, the wound closure rate of CNPs gel shows significant (12.27 %) wound closure as compared to the NC group and complete wound closure (100 %) on the 14th day, indicating accelerated wound healing. Conclusion: the present investigation endorses accelerated scar-free, accelerated wound healing potential of copper nanoparticles gel with anti-inflammatory potential

DEVELOPMENT AND CHARACTERIZATION OF SUSTAINED RELEASE METHOTREXATE LOADED CUBOSOMES FOR TOPICAL DELIVERY IN RHEUMATOID ARTHRITIS

Objective: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are essential part of the administration of Rheumatoid Arthritis (RA). Methotrexate (MTX) is effective for tumor necrosis factor alpha (TNF-a) biologic agents, indicated only in minority of patients suffering from severe RA. MTX remains the "anchor drug" in the treatment of RA. For delivery improvement, novel pharmaceutical drug delivery system i.e. MTX-Cubosomes were developed. Methods: Poloxamer 407 and Glycerol monooleate (Monoelin, MO) used and the formulation were characterized as a sustained release drug delivery system for Methotrexate. Different ratios of Monolein, Poloxamer 407 and water were used to develop the different cubosomes using homogenization and emulsification method. Characterization of formulations for morphology was performed and also particle size distribution by Transmission Electron Microscopy (TEM). Results: Formulation showed the internal cubic structures of the vesicles. The particle size of the formulations was found to be ranging from 53.21 to 185.32 nm, zeta potential of the formulations varied from-18.20-36.10 mV. The cubosomal formulation exhibited good entrapment efficiency along with high drug loading. Compatibility with the excipients was also established. An in vitro release study was done using Franz Diffusion cell indicated sustained release of the formulation at a rate of 1.25 %/h. Cubosomes proved to be reliable system for sustained transdermal drug delivery system. Conclusion: Methotrexate cubosomes is a novel medication delivery framework and in this examination it has been developed and characterized. The formulations were found to be promising in terms of its characterization parameters like particle size, zeta potential, entrapment efficiency, loading capacity, release kinetics, and stability, suitable for topical delivery

THERAPEUTIC EVALUATION OF CHEMICALLY SYNTHESIZED COPPER NANOPARTICLES TO PROMOTE FULL-THICKNESS EXCISIONAL WOUND HEALING

Objective: The purpose of this research was, synthesis of copper nanoparticles using environment friendly cementation method and evaluate their wound healing property on full-thickness excisional wound. Methods: Present study reports the synthesis of CNPs by single-step cementation method. Evaluation of CNPs was endorsed by morphological and chemical properties. Furthermore, CNPs was evaluated for its antibacterial potential and invitro hemocompatibility. Additionally, pharmacological evaluation of CNPs was assessed against excisional wound. Results: Characterization of final product indicate, particle size of CNPs were ranging from 100-150 nm. CNPs showed significant antibacterial activity (A= 2.1±0.1 mm, B =2.1±0.1 mm, C = 1.9±0.2 mm, at 10µg/ml), along with superior hemocompatibility (RBC cell survival 97±1 %). Further CNPs formulation shows increased level of anti-inflammatory cytokinin’s (IL-10, 42.7%) as compared to standard (STD), vehicle control, and normal control groups, attributed to accelerated wound healing (p<0.05 vs STD). Conclusion: The consequences the present investigation endorse the accelerated wound healing potential of CNPs with its anti-inflammatory potential

DEVELOPMENT AND EVALUATION OF DOXORUBICIN ANCHORED PLGA NANOPARTICLES AGAINST BREAST CANCER

The objective of this work was to design and develop Poly (D, L-Lactide-co-glycolide) (PLGA) nanoparticles (NPs) of Doxorubicin for the effective treatment of breast cancer. The nanoparticles (NPs) were optimized by applying a Box-Behnken design (BBD) using Design-Expert® Software and prepared using the double emulsification and precipitation method. Three independent factors such as PLGA 50:50 (A), PVA (B), stirring speed (C) were considered. Three dependent responses included entrapment efficiency (Response 1), particle size (Response 2) and Doxorubicin release at 10th hour (Response 3). ATR and DSC studies indicated compatibility between the drug and polymer. The morphological studies performed by SEM showed uniform and spherical shaped discrete particles with smooth surface and in a size range of 282.6 nm. X-ray diffraction was performed to confirm the crystalline nature of the drug after encapsulation. The NPs exhibited a zeta potential of 21.6 mV. In vitro release studies showed a drug release up to 10 hrs. The release kinetics study indicated first order kinetics while the release mechanism followed Higuchi model. The cell viability was found to be more than 80% after incubation with the DOX NPs for 24 h up to a concentration of 80 μg/ml. The DOX NPs treated MCF-7 displayed intrinsic cell damage and cell shrinkage as compared to the control group. It may be concluded from the present investigation that PLGA NPs bearing doxorubicin can effectively treat the breast cance

Formulation and Evaluation of Piroxicam Fast Dissolving Tablets Using Direct Compression and Sublimation Method

Objective: In the present research work, fast dissolving tablets of Piroxicam were formulated by two different techniques i.e. direct compression method and sublimation method using different superdisintegrants. Methods: Twelve formulations were prepared (PXM1 to PXM12) in which first six formulation were prepared by direct compression technique and other six formulation were prepared by sublimation method by using camphor as a sublimating agent. Result and Discussion: All the formulations were subjected for precompression, post compression parameters, and shows all the data within the specific limits. Formulation PXM4 containing 5 % crospovidone showed 99.480 ± 0.291 % drug release in 20 min which was more than the drug release of rest of the formulations. The optimized formulation PXM4 was compared with the marketed formulation and it revealed that drug release of PXM4 was found to be 99.397 ± 0.751 % in 20 min, which was greater than the marketed formulation. Finally, results were statistically analysed by the application of one way ANOVA and t-test. The stability study of the optimized formulation PXM4 showed no significant changes in, drug content, disintegration time and in-vitro drug release. Conclusion: Piroxicam can be successfully prepared using direct compression technique and it will enhance the drug dissolution, which will further increase absorption and bioavailability of the drug. Keywords: Direct compression, fast dissolving tablets, sublimation, Piroxicam

An Overview : Natural Bio-enhancer’s in Formulation Development

Bioenhancers are chemical entities that are obtained from synthetic as well as natural sources. They are mainly used in formulation development to enhance the bioavailability of poorly solubilized drug molecule. The ideal characteristic of bioenhancers includes inertness, nontoxic, cost effective and decrease the dose of active constituents. There are lots of natural bioenhancers available such as piperine quercetin niaziridin, genistein, glycrrhyzin, curcumin. The review focus on plant based bioenhancers and their active principle that produces those effects. There is a need of extensive study on natural bioenhancers which can be utilized in formulation development. Keywords: bioenhancer, bioavailability, piperine, curcumi

Cubosomes: A Novel Carrier for Transdermal Drug Delivery

Cubosomes are square and rounded particles with internal cubic lattice. Cubosomes are thermodynamically stable and consist of honeycombed (cavernous) structures separating two internal aqueous channels and a large interfacial area. Cubosomes are nanoparticles which are self assembled liquid crystalline particles of certain surfactants with proper ratio of water with microstructure that provides unique properties of practical interest. Bicontinuous cubic liquid crystalline phase is optically clear and very viscous material has the unique structure at nanometer scale. The word bicontinuous refers to the division of the two continuous but non-intersecting aqueous regions by lipid bilayer that is twisted into space filling structure. Hydrating a surfactant or polar lipid that forms cubic phase and then dispersing a solid like phase into smaller particles usually forms a cubosomes. Self-assembled cubosomes as active drug delivery systems are receiving more and more attention and interest after the first discovery and nomination. They exhibit different internal cubic structure and composition with different drug-loading modalities. It has high internal surface area and cubic crystalline structures, relatively simple preparation method, biodegradability of lipids, the ability of encapsulating hydrophobic, hydrophilic and amphiphilic substances, targeting and controlled release of bioactive agents. Cubosomes are having wide range of applications in various fields and they can be characterized by various evaluation parameters. So, Cubosomes are gaining more attention in pharmaceutical field. Keywords: Cubosomes, Liquid crystal, drug-loading, hydrophilic, hydrophobic, amphiphilic