Despite numerous research efforts, drug delivery through the oral route remains a major challenge to formulation scientists. The oral delivery of drugs poses a significant challenge because more than 40% of new chemical entities are practically insoluble in water. Low aqueous solubility is the main problem encountered during the formulation development of new actives and for generic development. A complexation approach has been widely investigated to address this issue, which subsequently improves the bioavailability of these drugs. This review discusses the various types of complexes such as metal complex (drug-metal ion), organic molecules (drug-caffeine or drug-hydrophilic polymer), inclusion complex (drug-cyclodextrin), and pharmacosomes (drug-phospholipids) that improves the aqueous solubility, dissolution, and permeability of the drug along with the numerous case studies reported in the literature. Besides improving solubility, drug-complexation provides versatile functions like improving stability, reducing the toxicity of drugs, increasing or decreasing the dissolution rate, and enhancing bioavailability and biodistribution. Apart, various methods to predict the stoichiometric ratio of reactants and the stability of the developed complex are discussed. 

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Drug complexes: Perspective from Academic Research and Pharmaceutical Market

Supramolecular ternary inclusion complexes of Irbesartan with hydroxypropyl-beta-cyclodextrin

A critical review on phytopharmacology, spectral and computational analysis of phytoconstituents from Streblus asper Lour



Regardless of the growing discovery of anticancer treatments, targeting cancer-specific pathways, cytotoxic therapy still maintained its abundant clinical significance based on the fact that tumours harbour a greater population of actively dividing cells than normal tissues. Conventional anti-mitotic agents or microtubule poisons acting on the major mitotic spindle protein tubulin have been effectively used in clinical settings for cancer chemotherapy over the last three decades. However, use of these drugs is associated with limited clinical utility due to serious side effects such as debilitating and dose-limiting peripheral neuropathy, myelosuppression, drug resistance and allergic reactions. Therefore, research initiatives have been undertaken to develop novel microtubule motor proteins inhibitors that can potentially circumvent the limitations associated with conventional microtubule poisons. Kinesin spindle proteins (KSP) belonging to the kinesin-5 family play a crucial role during mitosis and unregulated cell proliferation. Several evidences from preclinical studies and different phases of clinical trials have presented kinesin spindle protein as a promising target for cancer therapeutics. kinesin spindle protein inhibitors causing mitosis disruption without interfering with microtubule dynamics in non-dividing cells offer a potential therapeutic alternative for the management of several major cancer types and are devoid of side effects associated with classical anti-mitotic drugs. This review summarizes recent data highlighting progress in the discovery of targeted KSP inhibitors and presents the development of scaffolds, structure–activity relationships, and outcomes of biological, and enzyme inhibition studies. We reviewed the recent literature reports published over last decade, using various electronic database searches such as PubMed, Embase, Medline, Web of Science, and Google Scholar. Clinical trial data till 2021 was retrieved from ClinicalTrial.gov. Major chemical classes developed as selective KSP inhibitors include dihydropyrimidines, β-carbolines, carbazoles, benzimidazoles, fused aryl derivatives, pyrimidines, fused pyrimidines, quinazolines, quinolones, thiadiazolines, spiropyran and azobenzenes. Drugs such as filanesib, litronesib, ispinesib have entered clinical trials, the most advanced phase explored being Phase II. KSP inhibitors have exhibited promising results; however, continued exploration is greatly required to establish the clinical potential of KSP inhibitors.


Rinkal Chamariya

Papers

Supramolecular ternary inclusion complexes of Irbesartan with hydroxypropyl-beta-cyclodextrin

A critical review on phytopharmacology, spectral and computational analysis of phytoconstituents from Streblus asper Lour

Role of KSP inhibitors as anti-cancer therapeutics: an update