MIT-World Peace University (MIT-WPU) is a top educational institute located in Pune, India. It is recognized within&nbsp;UGC under Government of Maharashtra Act No. XXXV 2017.&nbsp;

It is part of the MIT group of institutions (established in 1983) which covers 10+ campuses across India and has more than 50,000+ students enrolled across various disciplines at a given point of time. The institute houses 15 schools ranging from Engineering &amp; Technology, Design, Pharmacy, Commerce, Governance among others. It offers undergraduate, postgraduate and PhD programs among different disciplines.&nbsp;

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MIT World Peace University

Pharmacy

Aim: To perform phytochemical screening, TLC, HPLC fingerprinting and antioxidant assay of Aqueous, Aqueous-Ethanolic and 95% Ethanolic extracts of Cissus repanda roots. Methods: Aqueous, Aqueous-Ethanolic and 95% Ethanolic extracts of Cissus repanda roots were subjected to preliminary phytochemical analysis. TLC patterns of all the three extracts were developed on the basis of phytochemical analysis results. All extracts were subjected to HPLC fingerprinting. The antioxidant potential of all the three extracts of Cissus repanda roots were evaluated by DPPH scavenging assay. Results: All three extracts showed the presence of various phytochemicals belonging to different chemical class viz. Alkaloid, glycosides, tannins, flavonoids, steroids and polyphenols. TLC fingerprinting of aqueous extracts showed presence of one distinct phytochemical with Rf value of 0.07 while Aqueous-Ethanolic extract showed three phytochemicals with Rf values of 0.11, 0.55, 0.95 and 95% Ethanolic extract showed two phytochemicals with Rf values of 0.16, 0.71. HPLC fingerprints of all extract showed four prominent peaks. Compounds showing peaks at 48.48 and 67.41 min. were found to be around 21.6 and 19.2% in the extract. All the extracts were subjected to antioxidant activity. Alcoholic extract of Cissus repanda roots showed highest antioxidant activity of 72.02% whereas Aqueous extract and Aqueous-Ethanolic extract showed 61.66 and 40.47% antioxidant activity respectively. Conclusion: The present study provides qualitative phytochemical analysis and antioxidant potential of Cissus repanda root extracts. HPLC and TLC fingerprint would be useful identification and isolation of therapeutically important phytochemicals. All extracts of Cissus repanda root showed good antioxidant activity.

World University root node

School of Pharmacy

Indian Journal of Pharmaceutical Education and Research

Phytochemical investigation, tlc-hplc fingerprinting and antioxidant activity of cissus repanda roots

Potential risk of agranulocytosis is one of the drug-induced adverse effects of the second-generation antipsychotic agents. The present investigation aimed to formulate and investigate olanzapine (OLZ)-loaded nanostructured lipid carriers (OLZ-NLCs) via intranasal (i.n.) route. The NLC was prepared by melt emulsification method and optimized by Box–Behnken design. Mucoadhesive NLC was prepared by using 0.4% Carbopol 974P (OLZ-MNLC (C)) and the combination of 17% poloxamer 407 and 0.3% of HPMC K4M (OLZ-MNLC (P+H)). The particle size, zeta potential and entrapment efficiency were found to be 88.95 nm ± 1.7 nm, − 22.62 mV ± 1.9 mV and 88.94% ± 3.9%, respectively. Ex vivo permeation of OLZ-NLC, OLZ-MNLC (P+H) and OLZ-MNLC (C) was found to be 545.12 $\mu$g/cm 2 ± 12.8 $\mu$g/cm 2 , 940.02 $\mu$g/cm 2 ± 15.5 $\mu$g/cm 2 and 820.10 $\mu$g/cm 2 ± 11.3 $\mu$g/cm 2 , respectively, whereas the OLZ-MNLC (P+H) formulation showed rapid drug permeation than the OLZ-NLC and OLZ-MNLC (C) formulations. The OLZ-MNLC (P+H) formulation was shown to have 13.57- and 27.64-fold more J ss than the OLZ-MNLC (C) and OLZ-NLC formulations. The OLZ nanoformulations showed sustained release of up to 8 h. Finally, the brain C max of technetium-99m ( 99m Tc)-OLZ-MNLC (i.n.) and 99m Tc-OLZ-NLC (i.v.) was found to be 936 ng and 235 ng, respectively, whereas the C max of i.n. administration was increased 3.98-fold more than the C max of i.v. administration. The in vivo hematological study of OLZ-MNLC (P+H) confirmed that the i.n. formulation did not reflect any variation in leukocyte, RBC and platelet counts. Hence, it can be concluded that the nose-to-brain delivery of OLZ-MNLC (P+H) can be considered as an effective and safe delivery for CNS disorders.

AAPS PharmSciTech

Agranulocytosis-Protective Olanzapine-Loaded Nanostructured Lipid Carriers Engineered for CNS Delivery: Optimization and Hematological Toxicity Studies

BACKGROUND: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis or spinal cord injury and treatment of muscle spasticity in spinal cord disease. Tizanidine hydrochloride belongs to BCS class II. It has low oral bioavailability and short half-life. Incorporating this drug in microemulgel is an excellent way to overcome problems associated with the drug. OBJECTIVE: Present research work was aimed to develop and optimize microemulsion based gel system for tizanidine hydrochloride. METHOD: Screening of oil, surfactant and co-surfactant was carried out. Ternary phase diagram was constructed to obtain concentration range of components. Prepared microemulsion was evaluated for pH, globule size, zeta potential, conductivity, density and viscosity. 32 level factorial design was applied to study effect of concentration of carbopol 934 and HPMC K15M on % cumulative drug release and viscosity of microemulgel using software Design Expert. Microemulgel was evaluated for pH, spreadability, viscosity, syneresis, drug content, bioadhesive strength, in-vitro as well as ex-vivo diffusion study. RESULT: Microemulsion was prepared by using isopropyl myristate as oil ,tween 80 as surfactant and transcutol P as cosurfactant. Largest transparent microemulsion region was found with Smix ratio of 1:1. FE-SEM showed globule size 28microm for batch B1 and zeta potential was -1.27mV indicating good stability of the microemulsion. Optimised batch was F6 which showed 92% drug release within 8 hours. It followed Korsmeyer-Peppas model. CONCLUSION: A stable, effective and elegant microemulgel formulation, exhibiting good in-vitro and ex-vivo drug release was formulated.

Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Optimization of Microemulgel for Tizanidine Hydrochloride

Quinoxaline, triazole and benzothiazole heterocycles plays an important role in modulating biological activity. The present work describes the biological evaluation of target molecules designed using autodock vina docker. Novel benzothiazole based [1, 2, 4]-triazolo [4, 3-a] quinoxalines were synthesized by condensation of substituted 2-amino benzothiazoles and 4-chloro triazoloquinoxalines. The synthesized compounds were characterized by analysis of physical and spectral data. All synthesized compounds were screened for antioxidant activity using 1, 1-Diphenyl-2-picrylhyrazyl radical scavenging, Hydrogen peroxide scavenging and Ferric reducing antioxidant power Method. The compounds 10g and 10i were found to be most active compounds of this series and other compounds showed moderate to less activity when compared with ascorbic acid. Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as antimicrobial, anti-inflammatory, anticancer and antidepressant, activity.

Indian Drugs

Design, synthesis, characterization and biological evaluation of novel benzothiazole based [1, 2, 4]-triazolo [4, 3-A] quinoxaline derivatives

Era has arisen to circumvent the application of conventional oral dosage forms and explore these novel drug delivery approaches to gain better benefits. Present investigation was carried out in the view to develop and characterize the mucoadhesive polymeric microparticles of mucilage obtained from natural resource i.e. Linum usitatissimum in order to prolong the release and overcome the drawbacks such as shorter half life and gastrointestinal irritation of dexibuprofen. L. usitatissimum mucilage was isolated and combined with sodium alginate for its fabrication into microparticles. Various batches were formulated and characterized, the results of FITR and DSC studies revealed the compatibility between drug and polymers. Apart from this, percent mucoadhesion was found to be in the range of 50-85%, whereas particle size was found in the range of 830-865 $\mu$m. Optimized formulation was successful in releasing the drug for the prolonged time period of 12 h. Overall study indicated that natural mucilage can be efficiently utilized to retard the drug release and minimize the side effects of the drug, so as to get maximum utilization of the therapeutic dose.

Latin American Journal of Pharmacy

Exploration of mucoadhesive microparticles by using Linum usitatissimum mucilage

Glioblastoma multiforme (GBM) is considered to be the most lethal primary brain tumor. Present research work is aimed to formulate teriflunomide (TFM) loaded intranasal (i.n.) mucoadhesive microemulsion (TFM-MME) and determined its efficacy against GBM. Globule size, zeta-potential and entrapment efficiency of developed formulation were found to be 22.81 ± 0.48 nm, −22.62 ± 1.1 mV and 98.88 ± 0.39%, respectively. Potential of TFM-MME was investigated in human U-87 multiform glioblastoma (U-87MG) cell line, where 73.2 ± 0.21% cells were destroyed at 160 $\mu$g/mL dose of the drug. Finally, C max values calculated for technetium ( 99m TC) labeled TFM in brain through administration of 99m TC-TFM-MME (i.n.) and 99m TC-TFM-ME intravenous (i.v.) using gamma scintigraphy and it was found as 0.62% and 0.41% RA/g, respectively. Thus, results suggested that 99m TC-TFM-MME (i.n.) is able to improve the uptake of TFM in brain approximately by 2-folds than 99m TC-TFM-ME (i.v.). Furthermore, drug targeting index (3.5), targeting efficiency (359.10%) and direct brain transport percentage (72.16%) confirmed drug targeting to the brain via nasal route. Concurrently, TFM-MME formulation didn't reflect any changes in liver biomarkers, hematology and histopathological examination in experimental animals. Hence, developed nose-to-brain delivery of TFM-MME can be a safe and novel brain targeting tool in brain disorders.

Journal of Drug Delivery Science and Technology

Intranasal teriflunomide microemulsion: An improved chemotherapeutic approach in glioblastoma

Neem oil gained importance due to its antibacterial properties. Therefore, it is extensively being used for various applications. Oils can be polymerized as a polyesteramide to extend their utility as biomaterials. In our studies, we synthesized polyesteramide from neem oil and various compositions of blends were prepared with the drug, chlorohexidine digluconate (CH) to develop a nanomaterial for tissue regeneration. The studies such as cytotoxicity, biodegradable, antibacterial, in vitro drug release, in vivo wound healing and histopathological studies were performed to identify their potential for tissue regeneration. In vivo wound healing studies of the nanofiber mats with and without CH recorded a faster healing rate as compared to the commercial cream (povidone-iodine). Most importantly, there was no requirement of repeated application of nanofiber mats during the treatment. The histopathology studies also suggested the re-epithelialization of the wounds. Hence, these nanomaterials are considered to be environmentally safe scaffolds for efficient tissue regeneration applications.

ACS Applied Bio Materials

Polyesteramide of Neem Oil and Its Blends as an Active Nanomaterial for Tissue Regeneration

The prodrug approach using various carriers has evolved as a significant tool in surmounting different obstacles in relation to drug formulation and targeting. Properties and selection of carriers or promoeities is a very important parameter in successful prodrug design. Carrier would change a drug's physical attributes in order to increase its fat or water solubility or to allow site-directed delivery. Though several studies have been carried out on various prodrugs, surprisingly very few reviews on different carriers, which can be used for prodrug synthesis were published to date. In this review different types of carriers, which can be used for prodrug synthesis are summarized. Examples of both marketed and investigational prodrugs using several promoieties are discussed with their advantages and future prospects. The present review is expected to be useful for scientists working in the field of drug discovery and development.

Indian Journal of Pharmaceutical Sciences

Carriers for prodrug synthesis: A review

A simple, rapid validated stability indicating HPTLC method for estimation of Salmeterol xinafoate was successfully developed. This method is based on HPTLC separation followed by UV detection at 252 nm. The separation was carried out on Merck TLC aluminium sheets precoated with silica gel 60F254 using Chloroform: Methanol: Ammonia (7:3:0.5 v/v/v) as a mobile phase and scanning was done by using TLC Scanner III. Salmeterol xinafoate gave well defined and sharp peak at Rf 0.52 ± 0.05 at 252 nm. Calibration curve was linear in range 1000-3000 ng/band for Salmeterol xinafoate. Stress degradation study includes hydrolysis under different pH, oxidation, thermal and photolytic conditions. The suitability of this HPTLC method for quantitative estimation of Salmeterol xinafoate was proved by validation in accordance with requirements of ICH guidelines Q2A (R1).

International Journal of Pharmaceutical Quality Assurance

Development and validation of stability indicating HPTLC method for estimation of Salmeterol xinafoate

Brain's biochemical integrity is very important for the physiological working of the central nervous system (CNS). Oxidative stress stands as one of the major factors causing cerebral dysfunction. When the antioxidant response mechanism fails to neutralize the oxidative stress conditions, the consequence leads to the generation of free radicals in excess. Since the brain constitutes lipid matter in abundance and also consumes oxygen in large amounts, it is vulnerable to oxidative stress. Thus, damage caused by oxidative stress to the brain results in a harmful influence on the normal physiology of CNS. Though the association of neurodegenerative illnesses (Alzheimer's disease, Parkinson's disease and Huntington's disease) with oxidative stress has been studied and also been reported, its participation in neuropsychiatric disorders like depression and anxiety are yet to be determined. The present chapter covers the discussion of cerebral oxidative stress, its consequence in impairing memory and the role of antioxidants in treating the memory impairment.