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A smart linker is a crucial element throughout the creation of polymer-drug conjugates. It binds different portions or subunits altogether and may be freed by a suitable trigger, resulting in localized drug distribution and enhanced bioavailability. PEG (Polyethylene Glycol) linkers can be synthesized chemically by specifically adding functionalized groups with chemical reactivity at certain structural ends of PEG. Because they may integrate a diverse range of groups, PEG linkers are frequently utilized in molecular biology experiments due to increased water solubility, excellent biocompatibility, and non-immunogenicity. In present work, we have included various linkers which are incorporated in design of PDC’s (polymer drug conjugates) of pegylated NSAIDs (nonsteroidal anti-inflammatory drugs) through PEGylation. The main focus was to investigate the pharmacodynamic changes brought about by these linker’s conjugated to model drug Ibuprofen (IB1-IB7). The tools used for the analysis are Argus Lab 4.0 for molecular docking and pkCMS as ADMET prediction tool. The outcome of this work was, establishment of a method for choosing suitable linker for designing PDC’s for various NSAIDs and other bioactive agents.

Reaction optimization has been a tedious task for the research chemist for very long and many approaches has been employed to achieve the best reaction condition resulting in highest yield. As an answer to this problem the statistical optimization approach has better chances of providing most acceptable solution to it. Through, our present work we have found that among other statistical approaches the custom design approach is the best methodology to be adopted for optimizing any synthetic reaction. The oxidative transformation of polyethylene glycol into polyethylene carboxylate by the use of TEMPO, NaClO and KBr; has been optimized by identifying the key factors affecting the yield and exact ratios of them to achieve highest possible yield. Here, we have employed custom design approach to further limit the experimental runs and yet find a better possible combination of reagents and conditions to get highest yield with maximum purity. This method has reduced the number of runs to only 16, which was 1024 in case of the traditional OVAT approach and in full factorial approach it was 64 runs. Thus, custom design method of DoE has been satisfactorily utilized for optimizing the oxidative derivatization of polyethylene glycol to polyethylene carboxylate.

Selection of a suitable nanocarrier with an ability to sense and respond to the biological signals is the most essential and challenging step toward the development of a promising targeted drug delivery system. The distinct and integrated physicochemical behavior of carbon nanomaterial presents it as a potential carrier system for site-specific delivery of various therapeutically active moieties including anticancer agents, anti-Alzheimer drugs, neuroprotective agents, antiinflammatory agents, and gene delivery. In addition, these are potentially used in tissue engineering and regenerative medicines. Surface functionalization of carbon nanomaterial is one of the indispensable prerequisites to facilitate drug loading, site-specificity, and safety of the carrier system. Recent investigations are evident that surface functionalization with various bioactives, proteins, peptides, and drug substances improve the therapeutic potency and reduce the toxicity of carbon nanomaterials. The current review article highlights carbon nanomaterial and its biomedical application, including surface functionalization via the covalent and noncovalent coupling. In addition, we have also briefly explained the toxicity profile of carbon nanomaterial.

Sixteen Schiff bases of quinazolin-4-one-linked 1,3,4-oxadiazoles were synthesized by reaction with different aromatic aldehydes. Purity of newly synthesized derivatives was confirmed through thin-layer chromatography, combustion analysis, and melting point. The structure of the derivatives was confirmed by determining infrared spectroscopy, nuclear magnetic resonance, and mass spectroscopy. All the synthesized derivatives were evaluated for their analgesic and anti-inflammatory activities in mice and rats, respectively. In animal studies, the derivative (E)-3-(5-(4-(4-methoxybenzylideneamino)phenyl)-1,3,4-oxadiazol-2-yl)-2-phenylquinazolin-4(3H)-one showed more potent analgesic activity and the derivative (Z)-3-(5-(2-(2-hydroxybenzylideneamino)phenyl)-1,3,4-oxadiazol-2-yl)-2-phenylquinazolin-4(3H)-one showed more potent anti-inflammatory activity as compared with other derivatives. The results of the present study indicate that reactions of 3-(5-(4-aminophenyl)-1,3,4-oxadiazol-2-yl)-2-phenylquinazolin-4(3H)-one and 3-(5-(2-aminophenyl)-1,3,4-oxadiazol-2-yl)-2-phenylquinazolin-4(3H)-one with different aromatic aldehydes produce Schiff bases of quinazolin-4-one-linked 1,3,4-oxadiazoles with potent analgesic and anti-inflammatory activities.

Plant-based medicines have been playing a pivotal role in the primary health care needs of humans since thousands of years. For the pharmaceutical industry, natural products serve as the best sources of therapeutic agents and drug leads. Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) is a phytoconstituent that was originally found in the plant genus Plumbago but is also present in Aristea, Aldrovanda, Dionaea, Drosera, Nepenthes, Drosophyllum, Dioncophyllum, Triphyophyllum, Ancistrocaldus, Ceratostigma, Diospyros, Juglans and others belonging to families like Iridaceae, Juglandaceae, Droseraceae, Nepenthaceae, Drosophyllaceae, Dioncophyllaceae, Anicistrocladaceae, Plumbaginaceae and Ebenaceae. It is noteworthy that the roots of Plumbago zeylanica have been used in Indian traditional medicine since more than 2500 years for the treatment of various diseases. In plants, plumbagin is biosynthesized as an acetogenic secondary metabolite. Several researchers successfully developed tissue culture methods for enhancing plumbagin production from the root and leaf culture of different species. Although synthetic chemists synthesized plumbagin via retro Diels-Alder and Diels-Alder reactions, a one-pot synthesis method may be used preferably for the large-scale synthesis of plumbagin. The bioavailability of plumbagin via oral route in rats was found to be 38.7 ± 5%. Due to greater lipophilicity, plumbagin shows extensive distribution into the body tissues with slow elimination rate. Plumbagin exhibits neuroprotective, antibacterial, antifungal, anti-leishmanial and anti-Helicobacter pylori activities. Moreover, it showed promising results in the treatment of a wide variety of cancers like lung cancer, ovarian cancer, breast cancer, leukemia, and prostate cancer. The anticancer effects of plumbagin are associated with modulation of various intracellular signaling pathways such as NF-kB, and AKT/mTOR, which play a crucial role in cancer cell proliferation, survival, invasion, and metastasis. Therefore, several laboratories have been engaged in exploring the therapeutic potential of plumbagin. While limited novel delivery strategies were adopted for plumbagin, there is a huge scope for the further development of novel formulations to enhance its therapeutic efficacy. This chapter covers the phytochemical, biotechnological and pharmaceutical aspects of plumbagin, which defiantly lighten the path of researcher aiming to work on this promising phytoconstituent.

In the present study, several new 1,3,4-oxadiazole derivatives linked with quinazolin-4-one moiety were synthesized by following steps. 2-methyl -4H-3, 1-benzoxazin-4-one, and 2-phenyl -4H-3, 1-benzoxazin-4-one were synthesized in the first and second step by stirring anthranilic acid in pyridine with benzoyl chloride and with an acetic anhydride for 30 min at room temperature. On treatment with semicarbazide with the above synthesized intermediates, that is, 2-methyl-4H-3,1-benzoxazin-4-one, and 2-phenyl-4H-3,1-benzoxazin-4-one in the third step afforded 2-methyl-4-oxoquinazoline-3(4H)-carbohydrazide and 2-phenyl-4-oxoquinazoline-3(4H)-carbohydrazide. These were introduced in cyclization reaction with different aromatic acids, aromatic aldehydes, and carbon disulfide in the next step, producing the corresponding 3-(4-acetyl-5-aryl-4,5-dihydro-1,3,4-oxadiazol-2-yl)-2-phenyl-quinazolin-4(3H)-one derivatives, 3-(4-acetyl-5-aryl-4,5-dihydro-1,3,4-oxadiazol-2-yl)-2-methyl-quinazolin-4(3H)-one derivatives, 3-(5-aryl-1,3,4-oxadiazol-2-yl)-2-phenylquinazolin-4(3H)-one derivatives and 3-(5-aryl-1,3,4-oxadiazol-2-yl)-2-methylquinazolin-4(3H)-one derivatives. Purity of these synthesized derivatives was confirmed by thin layer chromatography, melting point. Structure of the derivatives was set up by determining infrared spectroscopy, nuclear magnetic resonance, and mass spectroscopy. All the synthesized derivatives were evaluated for their analgesic and anti-inflammatory activities in mice and rats. In animal studies, the derivatives 3-[4-acetyl-5-(2-hydroxyphenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-2-phenylquinazolin-4(3H)-one and 3-[4-acetyl-5-(4-hydroxy-3-methoxyphenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-2-phenylquinazolin-4(3H)-one shown more potent analgesic activity and the derivatives 3-[4-acetyl-5-(4-methoxyphenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-2-phenylquinazolin-4(3H)-one and 3-[4-acetyl-5-(4-methoxyphenyl)-4,5-dihydro-1,3,4-oxadiazol-2-yl]-2-methylquinazolin-4(3H)-one shown more potent anti-inflammatory activity as compared to other derivatives. The results of current study indicate that cyclization of carbohydrazide group of intermediate 2-methyl-4-oxoquinazoline-3(4H)-carbohydrazide and 2-phenyl-4-oxoquinazoline-3(4H)-carbohydrazide with different aromatic acids, aromatic aldehydes, and carbon disulfide produces novel quinazolin-4-one linked oxadiazole derivatives with potent analgesic and anti-inflammatory activities.

Although plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) protects against cerebral ischemia and spinal cord injury-induced oxidative stress and inflammation by activating the nuclear factor-erythroid 2-related factor-2 /antioxidant response element (Nrf2/ARE) pathway, its role in the amelioration of neurodegenerative diseases remains unexplored. In the present study, we investigated the effect of plumbagin on Alzheimer’s disease (AD)-like condition in mice. The animals were treated intracerebroventricularly with streptozotocin (STZ; 3 mg/kg) twice, on day 1 and 3, to induce AD-like condition, and the symptoms were evaluated after 14 days. While the loss of learning and memory performance was evident in the mice subjected to Morris water maze (MWM), there was a striking increase in the population of astrocytes labelled with glial fibrillary acidic protein (GFAP) in the hippocampus. Daily intraperitoneal (i.p.) treatment with plumbagin (0.5 and 1 mg/kg), starting from 1 h prior to first dose of STZ, significantly prevented the cognitive deficits in MWM. On the other hand, administration of Nrf2/ARE pathway inhibitor, trigonelline (10 and 15 mg/kg, i.p.) enhanced the effects of STZ. Pre-treatment with subeffective dose of trigonelline (5 mg/kg) significantly attenuated the effects of plumbagin in MWM. While plumbagin prevented the STZ induced GFAP expression, this effect of plumbagin was attenuated by trigonelline. Moreover, the in silico docking study revealed potent inhibitory effect of plumbagin on β-secretase enzyme. The results of the present study suggest that plumbagin improves cognitive function in STZ induced mouse model of AD possibly via Nrf2/ARE mediated suppression of astrogliosis and inhibition of β-secretase enzyme.

Inspite of several dosage forms available in the market for effective localized action, the lozenges finds a special importance, as they are the best dosage forms for formulating large dose medicaments. The anatomy of mouth and cheek favors easy absorption of drug, reducing the systemic absorption thus ensuring a better patient compliance especially for pediatrics and geriatrics. Ascorbic acid mechanism of action suites this type of formulation and easily absorbed in oral cavity. Preformulation studies are primarily done to investigate the physicochemical properties of drug and to establish its compatibility with other excipients. Ascorbic acid was mixed with all excipients, used in the formulation in different. The formulated lozenges were evaluated for physical parameters and the results complied with the pharmacopoeiallimits.ascorbic acid hard candy lozenges were prepared by heat fusion method using sugar as a base. The usage of corn syrup in the formulation made the lozenges transparent and smooth, which helped in improving the elegancy of formulation. The controlled release of medicament from Lozenges was achieved by using polymers like methyl cellulose, locust bean gum, HPMC, K4M and xanthan gum. The prepared lozenges were subjected to physico-chemical as well as in vitro drug release study. Among all the formulations of hard candy lozenges FL1 showed good stability.

Monteleukast sodium is most commonly used in treatment of Asthma. It mainly prevents leukotriene mediated effect associated with asthama. Dispersible tablet are film coated or uncoated tablet that can be dispersed in liquid medium before administration, giving a homogenous dispersion. Dispersible tablet were prepared by using a direct compression method employing super disintegrating agentsuch as cross povidone, cross carmellose sodium and sodium starch glycolate, the tablet were preparedusing various diluents like MCC and lactose. Magnesium stearate and talc is used as a lubricant and glidant. Pre-compression parameter such as angle of repose, bulk density, tapped density, carrs index, hausner ratio carried out to study the flow properties of powder to achieve uniformity of tablet. The prepared tablet were evaluated for hardness, thickness, weight variation friablitity, % drug content, disintegration time and other parameter such as wetting time were also evaluated.

Herbal cosmetics are formulated, using different cosmetic ingredients to form the base in which one or more herbal ingredients are used to cure various skin ailments. The name itself suggests that herbal cosmetics are natural and free from all the harmful synthetic chemicals which otherwise may prove to be toxic to the skin. Compared to other beauty products, natural cosmetics are safe to use. Cosmeceuticals are cosmetic-pharmaceutical hybrid products intended to improve the health and beauty of the skin by providing a specific result, ranging from acne-control and anti-wrinkle effects, to sun protection. Calamine lotion is widely used as an antiseptic and protective for its cooling and soothing effect in various skin disorders. Instead of traditional synthetic products different plant parts and plant extracts are used in this study to procure calamine lotion having natural humectants, e.g. aloe-vera gel and honey. Herbal cosmetics are the preparations used to enhance the human appearance. The purpose of this study is to compare the semi synthetic activity of glycerin with other humectants in terms of their emollient properties to ensure whether calamine lotion can be formulated using natural humectants or not.