A CONCEPTUAL REVIEW ON TAILA MURCHANA

Taila kalpana has widely used dosage form described in Ayurvedic formulations for both external and internal use. Taila murchana is the first step of Taila preparation. Murchana has been adopted for enhancing the potency of oil and to remove the bad odour and Amadosa. In classics Tailas like Tilataila (sesame), Eranda (Castor) taila, Katu (Mustard) Taila needs Murchanaas preliminary process of Taila paaka. It has been mentioned in detail for the first time in Bhaishajya Ratnavali. Fat/Water soluble active principles of drugs are extracted into medicated oil in this method. Taila with Murchana are having more therapeutic potency and shelf life than crude Taila. The process of Murchana has high significance in today's scenario of globalization and the urge for better therapeutic efficacy. Hence the process of Murchana must be strictly included as the prerequisites of any medicated oil preparations. In this article an attempt has been done to review concepts regarding Taila murchana in literature of Ayurvedic pharmaceutics

Analytical assessment of Akika Pishti based on Ancient and Modern Parameters

Pishti Kalpana is one of the Kharaliya Kalpanas of Rasashastra which brings the heat sensitive substances to micro particle level without applying the heat for better therapeutic efficacy and is considered as Sukshma as Bhasma. In Rasa texts it is said that Marana of Ratna and Uparatna are not worthwhile hence, Pishti Kalpana is advocated. There is no direct reference for the Siddhilakshana of Pishti, but our Acharyas has mentioned that Pishti is a Anagnisidhdha Bhasma i.e. Pishti should be Bhasmavat, so the parameters mentioned for quality control of Bhasma in ancient text are applicable for assessing the Siddhilaxanas of Pishti. So an attempt has been made to study analytically Siddhilaxana of Pishti by both ancient and modern parameters with special reference to Akika Pishti. Akika is one of the semiprecious gem grouped under the Paradadi Varga, Uparatna Varga and Spatika Varga Ratna. In present study Pishti was prepared as per pharmacopeial standards and subjected to both ancient and modern tests to analyze viz. Pishtivarna, Mrudutva and Slakshanatva, Rekhapurnata, Varitara, Nirdhooma, Unama and Nischandratva tests according to classics and according to modern parameters like organoleptic tests, physio-chemical like LOD, pH, ash values, instrumental analysis like XRD , SEM-EDAX and particle size

Pharmaceutico Analytical Study of Mukta Shukti Bhasma

Background: Mukta Shukti is an aquamarine calcium carbonate compound. Mukta Shukti Bhasma is a classical ethical economical medicament, effective in general practice, pharmaceutical processing as per texts with systematic observation and technological updating is carried out in the present work. Objectives: To prepare Mukta Shukti Bhasma by different Pharmaceutical processes and carry out the analytical study. Materials and Methods: Grahya Ashodhita Mukta Shukti was subjected to Shodhana by Kanji Swedana for 3 hours and then divided into two parts. The first part of Shodhita Mukata Shukti was incinerated totally and after 1st Puta it was divided into two portions, first portion was subjected to Jala Bhavana and incinerated. The second portion was subjected to Kumari Swarasa Bhavana and incinerated. The second part of Shodhita Mukata Shukti was incinerated in Kumari Samputa and subjected to Kumari Swarasa Bhavana and incinerated until they attain Bhasma Siddhi Lakshanas and later all the three samples were subjected to analytical studies. Results: Mukta Shukti Bhasma by Jala Bhavana method, Kumari Bhavana method, and Kumari Samputa method requires 7, 6 and 3 Gajaputas respectively with an average of 324 cow dungs in each and at 793°C temperature. Conclusion: Kumari Bhavita Marana to Mukta Shukti leads to calcite form and Jala Bhavita Marana leads to calcium oxide hydrate form. Chemically Mukta Shukti Bhasma may be in both calcite and calcium oxide hydrate form, and XRD is a method in Standardization of Mukta Shukti Bhasma

A REVIEW ON THE ROLE OF NANOCRYSTALS AND NANOSUSPENSIONS IN DRUG DELIVERY SYSTEMS

Nearly 40% of drugs coming to the market nowadays are having poor solvency related issues and 70% molecules in discovery pipeline are in effect fundamentally insoluble in water. Nanocrystals is an unmistakable instrument to tackle the issue identified with poor fluid solvency and helps in improving the bioavailability of various drugs as presented in the literature. The particle size reduction came about into temperamental nanocrystalline system and the phenomenon of ostawald ripening happens. These techniques are preparing to the improvement of nanosized objects, which can play out multiple technological tasks. There are a few couples of noteworthy benefits of nanocrystal formulations, for example, upgrade oral bioavailability, improved dose proportionality, reduced food effects, appropriateness for administration by all routes and probability of sterile filtration because of diminished particle size range. One of the most adequate preferences of nanocrystals is their wide scope of utilization, for example, ophthalmic delivery, oral delivery, transdermal delivery, pulmonary delivery, intravenous delivery and targeted delivery, especially for tumour and brain. The increment in commercial value of nanocrystals just as the measure of nanocrystal products in the market is picking up more of attention to be utilized as a strategy so as to get commercial advantages. In this paper a brief and accurate precis of nanosuspension is stated with specific spotlight on nanosuspension preparation methodologies, benefits and few major applications of nanosuspensions

Maritoclax and Dinaciclib inhibit MCL-1 activity and induce apoptosis in both a MCL-1-dependent and -independent manner

The anti-apoptotic BCL-2 family proteins are important targets for cancer chemotherapy. Specific and potent inhibitors of the BCL-2 family, such as ABT-263 (navitoclax) and ABT-199, are only effective against some members of the BCL-2 family but do not target MCL-1, which is commonly amplified in tumors and associated with chemoresistance. In this report, the selectivity and potency of two putative MCL-1 inhibitors, dinaciclib and maritoclax, were assessed. Although both compounds induced Bax/Bak- and caspase-9-dependent apoptosis, dinaciclib was more potent than maritoclax in downregulating MCL-1 and also in inducing apoptosis. However, the compounds induced apoptosis, even in cells lacking MCL-1, suggesting multiple mechanisms of cell death. Furthermore, maritoclax induced extensive mitochondrial fragmentation, and a Bax/Bak- but MCL-1-independent accumulation of mitochondrial reactive oxygen species (ROS), with an accompanying loss of complexes I and III of the electron transport chain. ROS scavengers, such as MitoQ, could not salvage maritoclax-mediated effects on mitochondrial structure and function. Taken together, our data demonstrate that neither dinaciclib nor maritoclax exclusively target MCL-1. Although dinaciclib is clearly not a specific MCL-1 inhibitor, its ability to rapidly downregulate MCL-1 may be beneficial in many clinical settings, where it may reverse chemoresistance or sensitize to other chemotherapeutic agents

DEVELOPMENT OF pH-DEPENDENT CHRONOMODULATED DELIVERY SYSTEMS OF 5-FLUOROURACIL AND OXALIPLATIN TO TREAT COLON CANCER

Objective: To develop two different oral formulations such as 5-fluorouracil (5-FU) tablets and oxaliplatin (OX) microspheres which were further filled into capsules and coated with pH-sensitive polymer (eudragit S-100) for the chronotherapeutic treatment of colon cancer (Fluorouracil: Oxaliplatin regimen) to perform as a substitute for intravenous (IV) route based chronomodulated chemotherapy. Methods: The 5-FU tablet formulation was prepared with alginate and guar gum polymers in varied concentrations using wet granulation technique in two varieties such as granules coated and tablet coated formulations using eudragit RSPO as coating material to achieve controlled drug release. Alongside OX microspheres were formulated using the ionotropic gelation methodology in combination with alginate and chitosan polymers in varying concentrations to accomplish a time-controlled drug release. Prepared formulations were evaluated for pre-compression and post-compression parameters, percentage yield, percentage drug entrapment, Fourier transformed infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), In vitro and Ex vivo dissolution studies. Results: Pre-compression and post-compression parameters for 5-FU tablets were satisfied with Indian pharmacopeia specifications. The entrapment efficiency of OX microspheres were increased due to the elevated concentration of polymers up to a certain level as seen in A7M, further greater the concentration of polymer resulted in a decline of entrapment efficiency as seen in A4M and A8M. The optimized formulations A14T and A14M were shown in vitro drug release of 90.36 % by 24 h and 79.63 % by 9 h respectively. Conclusion: The two different oral formulations of 5-FU (Tablets) and OX (Microspheres) were found to be successful in controlled drug release. Therefore they can be efficiently used to control the rate of drug release to the colon in synchronization with the circadian timing system in the belief of improved therapeutic efficacy, tolerability and overall survival rate of cancer patients. Hence it is promised to be a better alternative for intravenous route based chronomodulated chemotherapy

ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF ACETYLSALICYLIC ACID VIA CO-CRYSTALLIZATION TECHNIQUE: A NOVEL ASA-VALINE COCRYSTAL

Objective: This study aims to synthesize acetylsalicylic acid (ASA) cocrystals using valine as a coformer via a co-crystallization technique to increase the solubility and dissolution rate of ASA. Methods: The ASA-valine cocrystal (1:1 molar ratio) was prepared using the solvent evaporation technique with ethanol: water (50:50). The cocrystal was characterized using Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), melting point to confirm the formation of cocrystal. The evaluation of cocrystal was done by drug content determination, solubility and dissolution studies. Results: The prepared cocrystal was successfully confirmed for the formation of a hydrogen bond. The melting point of prepared cocrystal was decreased compared to pure ASA and valine, which indicated the formation of a new crystalline form. The FT-IR studies showed the formation of a new hydrogen bond by shifting the-O-H,-C=O and-N-H functional groups. SEM studies ensured that the prepared cocrystals were in needle-like appearance. Finally, DSC and PXRD studies were also indicated the successful formation of ASA-valine cocrystal. The drug release of cocrystal was found to be 100% at 60th min. Where in the case of pure ASA and marketed product of ASA exhibited the dissolution rate of 59% and 69% at 60th min respectively. Conclusion: The co-crystallization technique can be adopted as the best strategy to increase the solubility and dissolution rate of BCS class 2 drugs. Therefore the prepared ASA-valine cocrystal can be a greater alternative to increase the solubility and dissolution rate compared with pure and marketed ASA