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Therapeutic effectiveness
Published in Dinesh Kumar Jain, Homeopathy, 2022
Now we should know how much time will be taken by a drug for its development? And what types of studies are required before successful development of a drug or treatment? Initial safety, biological effects, receptor study, enzyme inhibition and selectivity, drug absorption, metabolism, excretion, therapeutic efficacy, dose range, kinetics and adverse reaction, acute, subacute, chronic studies, effect on reproductive behavior, carcinogenic potential, mutagenic potential are studied and analyzed by clinical pharmacologist and physicians. Most new drug candidates are identified through chemical modification of known molecules, screening of natural products or previously discovered chemical entities for biological activity or rational drug design based on an understanding of biological mechanisms. Average ten years are taken by a drug before marketing and even after marketing surveillance is continued. If new toxicity appears after marketing, the drug is withdrawn from the market and the whole exercise of drug development becomes useless.
Granulation of Poorly Water-Soluble Drugs
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Albert W. Brzeczko, Firas El Saleh, Hibreniguss Terefe
Solid dispersion is one of the most important approaches employed in pharmaceutical product development to increase drug solubility and dissolution without a chemical modification of drug compounds. Compared with other conventional approaches, solid dispersion can reduce the size of drug particles to a much smaller level, even down to molecular dimension, and stabilize those physically modified compounds from agglomeration, crystallization, and phase separation through the understanding of the interaction between the drug compound and the carrier.
Manufacturing and standardizing allergen extracts in Europe
Published in Richard F. Lockey, Dennis K. Ledford, Allergens and Allergen Immunotherapy, 2020
Jørgen Nedergaard Larsen, Christian Gauguin Houghton, Manuel Lombardero Vega, Hendrik Nolte, Henning Løwenstein
The efficacy of allergen-specific immunotherapy, i.e., specific allergen vaccination, is related to the dose of vaccine administered, but the inherent allergenic properties of the vaccine imply a limitation due to the risk of inducing anaphylaxis. The risk of allergic side effects is minimized by administering repeated injections of increasing dose over time. Physical or chemical modification of the extract can further reduce this risk. Physical modification involves adsorption of the allergens to inorganic gels, such as aluminum hydroxide or alum, for the purpose of attaining a depot effect characterized by a slow release of the allergens. Chemical modification includes cross-linking of the allergens by treatment with aldehydes, such as formaldehyde or glutaraldehyde, for the purpose of reducing allergenic reactivity. Modified allergen vaccines are used for allergy vaccination but are not used for diagnosis since they were intentionally modified to reduce interaction with IgE.
Cell membrane-camouflaged PLGA biomimetic system for diverse biomedical application
Published in Drug Delivery, 2022
Jingjing Yan, Weidong Fei, Qianqian Song, Yao Zhu, Na Bu, Li Wang, Mengdan Zhao, Xiaoling Zheng
Chemical modification refers to the formation of covalent bonds between the reactive primary amines on the CM and the activated carboxylic acid, which enables the stable anchorage of functional molecules (Wang et al., 2015). To improve the penetration of the nanocarrier into the tumor tissues, Zhou et al covalently modified recombinant hyaluronidase (rHuPH20) with the amino group of living RBC in a two-step process via a cell-impermeable linker NHS-PEG-Maleimide with different linker molecule lengths (Zhou et al., 2016). The natural function of the RBCM was not compromised. PH20-RBCM-NPs enhanced NPs diffusion through extracellular matrix-mimicking gels and degraded the pericellular hyaluronic acid matrix of the PC3 cells. Interestingly, the long linker (MW: 3400) was more conducive to sustaining the enzyme activity than its short counterpart (MW: 425). The advantages of chemical grafting are that the density and length of the modified molecules are controllable, and the stable anchoring is particularly appropriate for biological macromolecules. However, the linkers must be carefully chosen to ensure that the conformation of the modified molecule or the biological function of the CM is not altered during the chemical reaction.
Lymphatic targeting for therapeutic application using nanoparticulate systems
Published in Journal of Drug Targeting, 2022
Nidhi Singh, Mayank Handa, Vanshikha Singh, Prashant Kesharwani, Rahul Shukla
In comparison to traditional based drug delivery system, nanotechnology assisted drug delivery system establishes quite unique and desirable properties. The delivery to lymphatic system can be achieved by two strategies i.e. pharmaceutical modification and chemical modification of drugs. In the chemical modification researchers enable the prodrug approach in which selective functional group is added to the drug for enhancing the bioavailability at desired site. Apart from this, in pharmaceutical approach cutting edge nanotechnology driven carriers are utilised. Furthermore, the oral administration, drug absorption takes place through enterocytes present in intestinal lymphatics. The systemic absorption is either by absorption through blood or lymphatic capillaries. The lymphatic system plays a vital role in the absorption of several drugs and facilitates targeted therapy. In the diseased state like inflammation and tumour metastasis mainly two mechanisms are involved in targeting to lymphatics, i.e. active and passive lymphatic targeting therapy [31].
Discovery of novel antischistosomal scaffolds from the open access Pandemic Response Box
Published in Expert Review of Anti-infective Therapy, 2022
Stefan Biendl, Cécile Häberli, Jennifer Keiser
Drug discovery for schistosomiasis, like many other neglected tropical diseases (NTDs), suffers from a lack of financial resources as well as insufficient drug-target information [10]. Screening small-molecule compound libraries in phenotypic drug activity assays can be cost-effectively employed to identify new starting points for structure–activity relationship studies, without the need for drug-target information [11]. Since drug candidates for schistosomiasis should be orally active, stable in warm and humid conditions as well as cheap to produce, it is advantageous to pre-select compounds on molecular characteristics for drug-likeness, such as the Lipinski rule of five [12]. This further increases the likelihood to discover suitable scaffolds that are amenable to chemical modification to improve pharmacodynamic or pharmacokinetic characteristics.