Current Drug Therapy - Volume 14, Issue 2, 2019

Background: Cancer is a havoc and killer disease. Several ways including allopathic chemotherapy have been used in the cancer treatment. Allopathic chemotherapy has several limitations and side effects. Unani medicine is also one of the therapies to cure cancer. Objective: In this type of treatment, herbal drugs are used for the treatment and prevention of cancer. The main attractive thing about herbal drug is no side effect as compared to allopathic chemotherapy. Methods: Actually, herbal drugs are the extracts of medicinal plants. The plant extracts are obtained by crushing and heating the main part of the plants; showing anticancer activity. The main plants used in the treatment of cancer are oroxylum indicum, dillenia indica, terminalia arjuna etc. Results: Mainly the cancers treated are of digestive system, breast, cervical, brain, blood, bone, lungs, thyroid, uterine, bladder, throat etc. Conclusion: The present review article discusses the importance of Unani system of medicine for the treatment of cancer. Besides, the future perspectives of Unani medicine in cancer treatment are also highlighted.

Background: Fluorinated substituents have played, and continue to play an important role in antitubercular drug design. Nonetheless, previous works have indicated that organofluorines like –F, CF3, -OCF3, and CHF2 etc have been used to modulate the pharmacodynamic and pharmacokinetic behaviour of antitubercular agents. Among the fluorinated groups, trifluoromethyl (-CF3) substituent is a very familiar pharmacophore used widely in antitubercular research. Objective: This review assesses the development of selected trifluoromethyl group bearing antitubercular agents that are either in treatment or considered to be potential. The prime objective of the present investigation was to provide initial evidences for the hypothesis that addition of trifluoromethyl group to antiTB agents could improve their potency. We also aimed to contribute to a better understanding of the role of trifluoromethyl group on drug-likeness antitubercular activity. Methods: In this review, we first brief out the possible effect of –CF3 substituent on pharmacodynamic and pharmacokinetic properties of drugs. Next, we turn to emphasize on the effect of trifluoromethyl substituent on different antitubercular scaffolds. Finally, we open the topic for the researchers to design potential antitubercular agents suitably substituted with fluorinated groups. Results: This review suggests that the replacement of –CF3 group in heterocyclic as well as phenyl ring led to the improvement in pharmacodynamic and pharmacokinetic properties of the compounds. Hence it's not surprising to see –CF3 group emerging as an alternative electron withdrawing group instead of halogens in many promising antitubercular agents. Conclusion: This unusual spectrum of advantage allied with its lipophilicity enhancing effect, made –CF3 group distinct from other substituents in modern antitubercular drug design. The present study provides conceptual advances to the understanding of the physicochemical properties of –CF3 group and its effect on antitubercular activity.

Background: Primary Parkinson syndrome is mostly treated by dopaminergic drugs, while the progression of the disease is not altered. Some non-dopaminergic are available, which are administered only after the Parkinsonian symptoms get worse. Objective: The objective of this review is to give basic results in order to compare a dopaminergic and non-dopaminergic pharmacotherapy in Parkinson’s disease and to control whether the add-on pharmacotherapy with non-dopaminergic drugs can inhibit the progression of the disease. Methods: In primary Parkinson syndrome, the altered activity of classical neurotransmitters and neuropeptides in the extrapyramidal system is summarized and up-dated. Anatomical studies on neural networks in the basal ganglia are mentioned. The direct, motor facilitatory pathway (D1 dopaminergic neurons) from the substantia nigra to the thalamus, via the internal globus pallidus, and the indirect, motor inhibitory pathway via D2 dopaminergic neurons have been considered. These established anatomical pathways have been brought in line with the neural interactions derived from neurotransmitter balances or imbalances. Besides, preclinical and clinical studies of effective non-dopaminergic anti-Parkinsonian drugs are reviewed. Results: It can be hypothesized that glutamatergic neurons enhance dopamine deficiency in the substantia nigra and putamen through an increased presynaptic inhibition mediated by NMDA receptors. In the putamen, 5-HT2A serotonergic neurons counteract D2 dopaminergic neurons and A2A adenosine neurons antagonize D2 dopaminergic neurons by activating glutamatergic neurons, which presynaptically inhibit via subtype 5 of metabotropic glutamatergic receptors, D2 dopaminergic neurons. In the extrapyramidal system, an up-dated neural network, which harmonizes established anatomical pathways with derived neural interactions, is presented. In Parkinson’s disease, a question should be answered, whether a combination of dopaminergic and non-dopaminergic drugs can promote an increased motor and non-motor functioning. Conclusion: A mono-target pharmacotherapy (using only dopaminergic drugs) and a multi-target pharmacotherapy (i.e. by combining dopaminergic and non-dopaminergic drugs) are compared. The alternate administration of dopaminergic and non-dopaminergic anti-Parkinsonian drugs, administered at different times during the day, must be tested in order to inhibit the progression of the disease. Assessment tools can be used to evaluate motor and cognitive functions. Moreover, imaging examination techniques can be also applied to control the course of the disease.

Background: Periodontal disease is an immuno-inflammatory condition of tissues that surround and hold the teeth. It is the disease which succeeds in all races, groups and both genders. Almost 10 to15% of the global population gets suffered from severe periodontitis as per WHO reports. Periodontal disease may likely cause other systemic diseases such as cardiovascular disease and pre-term low birth weight infants. Mechanical removal of plaques and calculus deposits from supra and subgingival environment is the backbone of periodontal treatment till date whereas complete elimination of these deleterious agents is quite unrealistic as the pocket depth increases. Recent Approaches: Recently controlled local drug delivery application is more encouraging in comparison to systemic approach as it mainly targets to enhance the therapeutic efficacy by maintaining site-specificity, avoiding first pass metabolism, reduction in gastrointestinal (GI) side effects and decreasing the dose. Several drugs such as antiseptics and antibiotics alongwith various carriers are being formulated as local drug delivery systems for effective management of the disease. Various local delivery systems reported are fibers, films, strips, compacts, injectables, microparticles, vesicular carriers, gels and nanoparticles. These local carriers provide effective prolonged treatment at the site of infection at reduced doses. This review enlightens detailed pathophysiology and various phases of periodontitis, challenges in treatment of disease and various antimicrobial agents (along with their marketed formulations) used. The main emphasis of the review is to cover all carrier systems developed so far for local delivery application in the effective management of periodontitis, as a patient compliant drug therapy.

Background: The increasing complications associated with hypertension often require a combination of two or more drugs acting through different routes to counter the elevated blood pressure. Objective: The present investigation envisaged at preparing and evaluating a transdermal formulation containing gelled microemulsion drug in adhesive (DIA) patch for simultaneous systemic delivery of valsartan and nifedipine aimed at effective management of hypertension. Methods: An optimized microemulsion was prepared by using Captex® 500 (7.34% w/w), Capmul® MCM (4.24% w/w), Acrysol EL 135 (24.43% w/w), Transcutol P® (5% w/w) and water (58.9% w/w). Gelling was contributed by polyvinylpyrrolidone K 90F and polyethyleneimine where the latter also conferred skin adhesion properties to the patch. DIA patches were evaluated for in vitro drug release as well as in vivo pharmacokinetics and pharmacodynamics in rats. Results: In vitro permeation of nifedipine or valsartan from the selected DIA patch was 10.67-fold and 1.25-fold higher as compared to their aqueous dispersions. The relative bioavailability of nifedipine was 1.34 and that of valsartan was 2.18 from this DIA patch with respect to the oral administration of their aqueous suspension. Conclusion: Transdermal delivery of either drug alone was not effective in reducing methyl prednisolone acetate-induced hypertension, whereas, simultaneous transdermal delivery of both drugs from DIA patch effectively maintained systolic blood pressure at a normal level in these rats for 20 h.

Objective: The prime objective was to formulate pellet formulation incorporating a newer extrusion- pelletisation aid, Pregelatinised Starch (PGS) and to scrutinise the factors that can affect the quality of the pellets and to overcome the slower disintegration of Microcrystaline Cellulose (MCC). Methods: Pellets were prepared initially using PGS, MCC, water, ethanol, HPMC K 4 M and Febuxostat was employed as model drug. Optimisation of formulation was done by employing Quality by design (QbD) and Design of experiment (DoE) approach. Ratio of PGS and MCC, ratio of binder and spheronisation speed were selected as independent variables and disintegration time and % cumulative drug release as dependent variables. In vitro in vivo correlation of the optimised batch was carried out using Wagner nelson method. Incompatibility studies have indicated compatibility of drug and excipients. Results: From the experiments, it was proved that the batch comprising 3:1 ratio of PGS and MCC, 1:1 binder solution and 1500 speed yielded good pellets with decreased disintegration time and improved dissolution rate as compared to pure Febuxostat. IVIVC studies indicated one to one correlation between in vitro and in vivo parameters. Conclusion: Pellets with good quality, minimum disintegration time and improved dissolution of model drug were successfully prepared with maximum amount of PGS. Optimisation using QbD approach was worth fruitful that affected the quality of pellets.