International Journal of Pharmaceutical Sciences and Drug Research

1-6

Authors: Pawan Kumar1, Shailendra Kumar Singh1*, Deepak Kumar Jindal1, Vandana Handa2, Jyoti Bilonia3

Alopecia areata is a common, chronic inflammatory disease, characterized by patchy hair loss on the scalp, affecting about 2.1% of world population. Presently, minoxidil has been used for treatment of alopecia as topical lotion, but associated with many drawbacks like systemic side effects and low contact time with skin. Therefore, in the present work, minoxidil gel was prepared using a novel copolymer, Sepineo P 600 to overcome these drawbacks. The prepared gel was characterized for pH, drug content, viscosity, spreadability, skin adhesivity, occlusivity, in vitro drug release, ex vivo skin permeation, stability and finally for skin corrosivity. The drug content of the finalized gel was found to be 99.80 ± 0.82%. The formulation showed good spreadability, occlusivity, adhesiveness and viscosity. In vitro release studies showed that the drug release from prepared gel followed matrix release pattern as compared to lotion. Mathematical modelling of the drug release data suggested Higuchi release model. The formulated minoxidil gel was found to be non-corrosive and stable when subjected to accelerate as well as real time stability studies. Overall, the minoxidil gel formulation was suitable for skin application and can be an effective dosage form for the treatment of Alopecia areata.

12-19

Authors: G. Demirel*, D. Saray, B. Yaman, A. Turkyilmaz

Quality by Design (QbD) is well established in the pharmaceutical industry for pharmaceutical development and manufacturing processes. The knowledge obtained during development may support the establishment of a design space and determines suitable process controls. This same QbD principle has been applied to the development of analytical methods and is termed “Analytical Quality by Design” (AQbD). Analogous to process QbD, the outcome of AQbD is well understood, fit for purpose, and robust method that consistently delivers the intended performance throughout its life cycle. The present work is aimed to develop an AQbD approach to analytical method development and validation based of Tadalafil and its impurities by the NP-HPLC method. The other objective of this work is to establish an in-depth understanding of the method and build in the quality during the method development to ensure optimum method performance over the lifetime of the product.

27-30

Authors: C. Mamatha*, M. Thangavel

Otitis media is the infection of the middle ear, caused as a result of the infection of the fluid built up in the tympanic cavity, mainly by bacteria even though viral and fungal otitis media has been reported. The bacterial isolated from the otitis media patients are known to be biofilm producers and hence the success in causing recurrent ear infections and so the detection of biofilms becomes essential as only then can effective treatment strategy be planned. As such, this paper is dedicated to finding the best method for the detection of biofilm producers in the case of otitis media causing bacteria.

39-45

Authors: Amol Bhalchandra Deore1*, Vinayak Dnyandev Sapakal2, Nilofer S. Naikwade3

To investigate the antidiabetic, antihyperlipidemic and renal protective activities of the aqueous and ethanol extract of Garcinia indica fruit rinds against alloxan induced diabetes in rats. Wistar rats were made diabetic by a single dose of alloxan hydrate [130 mg/kg i.p.]. After the successful induction of experimental diabetes, rats were divided into five groups each comprising a minimum of six rats. The effects of extracts and glibenclamide on fasting blood glucose, plasma lipid levels and renal profile were examined for 21 days. Blood glucose levels and biochemical parameters such as serum cholesterol, triglycerides, HDL-cholesterol, LDL-cholesterol, urea and creatinine levels of rats were measured using on weekly intervals i.e day 0, 7, 14 and 21 after daily administration of all extracts at dose of 500 mg/kg. Statistical analysis was performed using Dunnett’s test. p<0.01 was taken as the criterion of significance. Oral administration of both aqueous and ethanol extract for 21 days caused a significant [p<0.01] reduction in blood glucose levels, lipid profile except HDL; urea and creatinine in diabetic rats. Garcinia indica fruit rind possesses antihyperglycemic activity as well improves total lipid levels and renal profile. It can justify folklore uses of the plant in diabetes.

286-290

Authors: Neha Jain*, Mohan Lal Kori

The objective of the present study is to evaluate the quality of the marketed and self collected samples of Plumbago zeylanica L. roots on the standardization parameters. This study is planned mainly to confirm changes with quality of drug. Now a day’s more demand of herbal drugs for disease treatment, lack of knowledge of proper methodology and availability are promoting the practices of adulteration and substitution. Thus, the standardization of the plant crude drugs is necessary to maintain their therapeutic efficacy. Comparative studies were carried out to evaluate the standards of P. zeylanica L. with emphasis on organoleptic evaluation, physicochemical and phytochemical analysis. Samples were procured from local market and self collected to determine the qualitative and quantitative variations. The result indicates that self collected sample showed significant results with comparison to marketed sample.

299-307

Authors: A. Deevan Paul*, P. Samatha, S. Manasa, R. Munemma, D. Supriya

Oral mucosal drug delivery system is widely applicable as novel site for administration of drug and controlled release action by preventing first pass metabolism and enzymatic degradation due to GI microbial flora. The oral cavity represents a challenging area to develop an effective drug delivery modelling. This arises due to the various inherent functions of the oral cavity (eating, swallowing, speaking, chewing), as well as the presence of the fluid that is involved in all these activities, saliva. This fluid is continually secreted into and then removed from the mouth. Oral Mucosa drug delivery system provides local and systemic action. The delivery of drugs through the buccal mucosa has attracted much research interest over the past two decades and numerous approaches, both conventional and complex, have been developed in an attempt to deliver a variety of pharmaceutical compounds via the buccal route. To outline the progress in the in vitro and in vivo modeling of Mucosal drug delivery and provide a critical review of currently used methods. The purpose of this review is to represent the modeling of oral cavity with Mucoadhesive drug delivery systems and clarify the potential alternative to conventional therapy.

315-322

Authors: P Poornima1*, K Abbulu2, K Mukkanti1

The present study was focused on Gastro-retentive tablets of Quetiapine fumarate using hydrophilic polymers HPMC K 250 PH PRM, HPMC K 750 PH PRM and HPMC K 1500 pH PRM as release retarding agents. WSR 301 was chosen as resin, Sodium bicarbonate was used as effervescent agents. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. The tablets were prepared by direct compression method and the release rate was found to decrease with proportional increase in the ratio of polymer to drug. Quetiapine fumarate has good water solubility and is absorbed well from stomach and therefore is a very good drug to be formulated into gastro retentive floating dosage form. In-vitro release profile of Quetiapine fumarate and marketed product when compared, the optimized formulation F19 showed drug release of 98.61% within 24 h whereas 96.78% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non fickian transport by coupled diffusion and erosion. Such a formulation of Quetiapine fumarate with extended drug release over 24 hours probably is the best formulation for the treatment of Schizophrenia with only one oral tablet a day thus minimizing the side effects with low drug dose. The optimized formulation remained stable when subjected to accelerated stability studies.

327-333

Authors: S. Jyothi Sri1, D.V.R.N Bhikshapathi2*

The present investigation was aimed with the objective of developing fast dissolving oral films of Aripiprazole to attain quick onset of action for the better management of Schizophrenia. Fourteen formulations (F1-F14) of Aripiprazole mouth dissolving films by solvent-casting method using HPMC E5, HPMC E15, Maltodextrin, PG and PVA. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F13 showed minimum disintegration time 10 sec, maximum drug was released i.e. 99.49 ± 0.36% of drug within 8 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions take place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 20.73 ± 0.25 after 8 min. Therefore, it can be a good alternative to conventional Aripiprazole for immediate action. In vitro evaluation of the Aripiprazole fast dissolving oral films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Aripiprazole. The mouth dissolving film is potentially useful for the treatment of Schizophrenia where the quick onset of action is desired.

210-213

Authors: Megha Shukla, Sumeet Kaur Bhatia, Balbir Kaur*

This research article describes the synthesis of phenyl hydrazone derivatives of 5-acetyl-6-methyl-4-substituted phenyl-2-thioxo-1,2,3,4-tetrahydropyrimidines, as no derivatization has been reported at carbonyl functionality at position 5 of corresponding rings till date. The prepared derivatives were characterised using modern spectral techniques and were screened for their in-vitro anti-microbial activities by agar diffusion method. Among synthesised derivatives [II(a-g)], compound II(f) was found to be the most potent anti-bacterial agent and rest of the compounds had shown moderate to weak anti-bacterial activity.

220-223

Authors: Atreyee Sarkar*, Mrunal S Davey, Atul Savalia, Shivanand Dhanure

Pyrazinamide is a widely used drug for the treatment of tuberculosis. A 150 mg Dispersible Tablet (DT) formulation of the drug was prepared by Micro Labs, a generic drug company. The formulation was developed for easy administration into paediatric patients. It was tested for bioequivalence in healthy adult human volunteers in fasting condition. A total of 36 subjects were enrolled in the study and all the 36 subjects completed both the two periods of the study without showing major adverse events. The pharmacokinetic parameters determined for bioequivalence were Cmax and AUC0-t. The two parameters were within the limit of bioequivalence criteria. The 150 mg DT formulation developed by Micro Labs was found to be bioequivalent to 500 mg immediate release tablet formulation of Riemser Pharma. Both the formulations were safe and well tolerated among the tested human subjects. No major adverse events were observed.

228-233

Authors: Md. Muzaffar-ur- Rehman1*, G. Nagamallika2

A simple, rapid, precise, and accurate RP-HPLC method for the estimation of Ivabradine Hydrochloride an anti-anginal agent, both as a bulk drug and in pharmaceutical formulation was developed. The chromatographic separation was achieved on a Thermosil C18 150 × 4.5 mm, 5μm column by using a mobile phase containing a mixture of methanol and phosphate buffer pH 6.5 in the ratio of 65:35 % v/v at a flow rate of 1ml/min and at an ambient temperature. The detection was monitored at a wavelength of 265nm. A clear chromatographic peak was identified with the retention time of 4.36 min and tailing factor of 1.23. The developed method was validated according to ICH guidelines with respect to specificity, linearity, accuracy, precision and robustness. The method shows a good linear relationship with correlation co-efficient of more than 0.992 in the concentration range of 30µg-150µg. The method showed mean % Recovery of 100.4% and %RSD for repeatability and intermediate precision was less than 2%. The proposed method can be used successfully for the quantitative determination of Ivabradine HCL in pharmaceutical dosage forms.

240-246

Authors: Sunidhi Mahant*, Shivali Singla, Sachin Goyal, Bhimi Kumari, Abhishek Soni

Mouth dissolving tablet is an innovative solid unit dosage form that overcome the problem of swallowing and provide rapid disintegration & dissolution to release the drug as soon as they come in contact with saliva, hence provide quick onset action. The aim of this study was to formulate & evaluate mouth dissolving tablets of Ondansetron hydrochloride using natural super disintegrating agent. Ondansetron hydrochloride is a serotonin receptor (5-HT3) antagonist used to treat nausea and vomiting arises during chemotherapy and radiation therapy. Mouth dissolving tablets were prepared by direct compression method using natural super disintegrating agent (Plantago ovata mucilage). Prepared tablet were evaluated for Hardness, weight variation, friability, thickness, wetting time, dispersion time, water absorption ratio, disintegration & dissolution study. According to results of optimized batches it has been concluded that Formulation batch F6 was an ideal batch which contain 12% w/v concentration of Plantago ovata mucilage showed least disintegration time that is 7 seconds & maximum drug release of (98.57%) within 15 minutes and was best among all the formulations.

252-255

Authors: Sanjay Jain1*, R. K. Maheshwari2, Rajesh Kumar Nema3, Indrajeet Singhvi1

Commonly used organic solvents for spectrophotometric analysis of water insoluble drugs are methanol, ethanol, chloroform, benzene, toluene etc. The main drawbacks of organic solvents include high cost, toxicity, and pollution. Organic solvents have numerous adverse effects caused by single exposure like dermatitis, headache, drowsiness, nausea, eye irritation and long term exposure causes serious effects such as neurological disorder, chronic renal failure, and liver damage. They should be replaced by other ecofriendly alternative sources. The present study is an attempt to show that solid can also be used to act as solvent precluding the use of organic solvents. A simple, safe and sensitive method of spectrophotometric determination of Ondansetron hydrochloride obeyed beers law in the concentration range of 10-50µg/ml at 310 nm. The results of analyses have been validated statistically for linearity, accuracy, precision, LOD and LOQ. The results of validation parameters also indicated that proposed method was found to be accurate, precise, reproducible, sensitive, and suitable for routine quality control analysis for estimation of Ondansetron Hydrochloride in solid dosage formulation.

263-267

Authors: Vineela Satuluri*, Vidyadhara Suryadevara, Vijetha Pendyala, Narasimhareddy M

Thrombotic disorders like myocardial and cerebral infarction are fatal blood clotting related diseases. Synthetic therapeutics used in such disorders has serious adverse effects, so there is a need to investigate some more safe natural thrombolytic agents. Present study is a preliminary work towards such endeavors. During this study analysis of thrombolytic activity and anti-inflammatory activity of Thespesia populnea leaf extract using a simple and quick in vitro clot lysis assay was performed. Various concentrations of leaf extract i.e. 200µg/ml; 400µg/ml and 600µg/ml were tested at various time intervals including; 24, 48 and 72 hours duration of incubation at 37°C for observing maximum clot lysis. The result findings indicated that concentrations of leaf extract enhanced the percentage of clot lysis in dose dependent manner along with the incubation time factor. However; streptokinase SK a reference standard and water were used as a positive and negative control showed clot lysis maximum 96.35% and 35.22% in 72 hours of incubation respectively. Alcohol extract of whole plant of Thespesia populnea (Family: Malvaceae) was assessed for its anti-inflammatory activity by in vitro methods. In vitro anti-inflammatory activity was evaluated using albumin denaturation assay at different concentrations. Diclofenac sodium was used as standard drug. The results showed that Thespesia populnea alcohol extract at a concentration range of 400-1600µl significantly protects from protein denaturation.

275-279

Authors: Arun Mahato1*, Birendra Shrivastava2, Nithya Shanthi1

In our effort to identify potent anti-inflammatory and analgesic agents a number of 7-chloro-3-substituted-2-phenylquinazolin-4(3H)-ones have been synthesized starting from 4-chloro anthranilic acid. Docking analysis of the quinazolinone derivatives were done with COX-II protein which was carried out by means of the AutoDock program. Their structures have been elucidated on the basis of elemental analyses and spectroscopic studies (IR, 1H-NMR, MS). The synthesized compounds were tested for their analgesic activity by tail-flick method and anti-inflammatory activity by carrageenan induced rat paw oedema method. Preliminary evaluation of the anti-inflammatory and analgesic properties of the prepared compounds has indicated that some of them exhibit moderate to significant activity, compared to diclofenac standard.

149-159

Authors: SK Nagar1*, MM Soniwala2

The purpose of this investigation was to increase the solubility and dissolution rate of Cilnidipine by the preparation of nanosuspensions with solvent antisolvent method at the laboratory scale. Drug solution of Cilnidipine in acetone this mixture was added to stabilizer solution under continuous homogenization. Central composite design was employed to study the effect of the independent variables on the dependent The relationship between the dependent and independent variables was further Elucidated using multiple liner regression analysis (MLRA) and contour plots. Various process and formulation parameters were screened like homogenization speed, solvent to antisolvent ratio, homogenization time, type of stabilizer, concentration of drug and concentration of stabilizer. Physical stability can be enhancing physical stability of this colloidal system; nanosuspensions were freeze dried using D-mannitol. Seven different stabilizers were tried. Among them Poloxamer 407, Poloxamer 188, PVA and Tween 80 yielded nanosuspension in range of 90 to 350 nm. Freeze dried nanosuspensions were filled in capsules to make a deliverable dosage form and almost 100% drug dissolved in 5 minutes. The outcome of this study reveals the immense potential of nanosuspensions for delivery of Cilnidipine by improving its solubility and dissolution rate. These results show that the preparation of Cilnidipine-loaded nanosuspensions significantly improved the in vitro dissolution rate, thus possibly enhancing the fast onset of therapeutic drug effect.

169-177

Authors: Umang Motka1, Mahesh Dabhi1, Navin Sheth2, Ashvin Dudhrejiya3*

Isradipine is a poorly water soluble antihypertensive drug has low bioavailability. The aim of this study was to formulate and characterize isradipine nanosuspension to enhance the solubility of isradipine and thus its bioavailability. Media milling technique was used for the formulation of nanosuspension. The effects of different important process parameters, i.e. the selection of stirring time, selection of concentration of zirconium beads, stirring speed were investigated by preliminary studies while concentration of stabilizers were optimized by simplex lattice design. Concentration of HPMC E3 LV(X1), Carbopol 934P(X2) and PVP K25(X3) were selected as the independent variables whereas mean particle size (Y1), saturation solubility (Y2) and cumulative percentage drug release (cpr) (Y3) were selected as dependent variables. The optimized batch had 100% w/v of zirconium beads, 0.5%w/v of PVP K25 as stabilizer, 0.1%w/v of isradipine, 15 ml of distilled water and 20 hours of stirring time. The particle size and zeta potential of optimized nanosuspension were 248.6 ± 20 nm and 13.96 ± 5 mV respectively. The size of particles of nanosuspension was measured by particle size analyser and transmission electron microscopy (TEM). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) analysis indicated that there was no interaction between drug and stabilizers. The saturation solubility and in vitro dissolution rate of isradipine was significantly increased by particle size reduction and which may leads to increase the bio-availability of the Isaradipine. The stability study of the formulation was carried out for a period of 12 months.

182-186

Authors: Harleen Kaur*, Sunil Kumar Bose, Anitha Vadekeetil, Geeta, Kusum Harjai, Richa

Achillea filipendulina is an aromatic plant of family Asteraceae with bright yellow colour flowers. The objective of the study was to extract the essential oil from the flowers of the selected plant using Clevenger apparatus, to analyse the chemical composition of the oil using GC-MS and to screen the essential oil for its antibacterial property against both gram-positive and gram-negative bacteria. GC-MS results revealed that the main chemical constituents present in the oil were trans 2,7 Dimethyl 4,6 octadien-2-ol (27.93%), borneol (21.44%) and santolina triene (7.13%). The results of agar well diffusion assay revealed that the oil showed antibacterial activity against all the tested bacteria except Pseudomonas aeruginosa. Minimum inhibitory concentration (MIC) of oil was determined against the sensitive bacteria. MIC values against Staphylococcus aureus and Escherichia coli were similar (0.312% v/v) and for Bacillus cereus, MIC value was found to be (0.156%). Results indicated the great antibacterial potential of oil of this plant against gram positive and gram negative bacteria.

195-200

Authors: Animeshchandra G. M. Haldar1*, Santosh S. Chhajed2, Debarshi Kar Mahapatra3, Kanhiya M. Dadure4

In the present investigation, the synthesis of few novel leads bearing 2-(p-hydroxyphenyl)-4–(substitutedphenyl)-1H-1,5–benzodiazepine pharmacophore is described. The substituted chalcone and their derivatives 3(a-j) were synthesized by base catalyzed Claisen-Schmidt condensation between p-hydroxy-acetophenone and appropriate aldehydes. The dibromostyryl ketones 4(a-j) were obtained by the reaction the chalcone with bromine in acetic acid. The dibromostyryl ketone were reacted with methanol in presence of sodium methoxide followed by acidic hydrolysis give 1-(4-hydroxyphenyl)-3-(substitutedphenyl)-1,3-propanediones. The targeted compounds; the substituted 1,5-benzodiazepines were synthesized with o-phenylenediamine and synthesized 1,3-propanediones. The structures of synthesized compounds were confirmed by spectroscopic and analytical techniques (IR, 1H-NMR, and MS). The free radical scavenging activity of the synthesized analogs was monitored by in vitro antioxidant activity protocol. The derivatives 6f, 6g, 6i, and 6j were found to exhibit good antioxidant activity with 59.07%, 41.33%, 68.3% and 60.4% scavenging activity respectively as compared to standard ascorbic acid which demonstrated 79.73% activity. The current research revealed the potential of 2-(p-hydroxyphenyl)-4–(substituted-phenyl)-1H-1,5–benzodiazepine as emerging free radical scavengers. The study helped to establish a structure-activity relationship (SAR) where the substitution on the phenyl moiety of the 1,5-benzodiazepine was found to play profound role and influence over biological activity. The research will open new avenues for the development of antioxidant moieties having perspectives in cancer, inflammation, and several other ailments.

100-104

Authors: Babu A, Sheik Noor Mohamed M, Jaikumar K, Anand D, Saravanan P*

Traditional healers possess a rich knowledge on the use of medicinal plants for the treatment of various diseases. Enicostemma axillare (Lam). Raynal is one plant, used by healer to treat gastric cancer or ulceration. We assessed the phytochemical components of leaf extract for its antibacterial activity, to add value and provide an evidence-base for their traditional use. The antibacterial potential of the leaf extract was tested against Helicobacter pylori using agar well diffusion method. The minimum inhibitory concentration (MIC) of ethanol extract exhibited the (MIC) against H. pylori ranged from 200µg/ml - 250µg/ml followed by chloroform extract. Gas chromatography and mass spectrum (GC-MS) analysis confirms the occurrence of different components in the ethanol and chloroform leaf extract of the studied species.

113-117

Authors: Anantha Padmanabhan S, John Wyson W, Marimuthu S, Saravanan P, Anand D*

Microbial community has been a major part in the drug industry. They are known for their effectiveness and do not cause any undesirable effects. Exploitation of bacteria could be fruitful for mankind. Bacteria play a major role in producing useful bioactive compounds. HSV-1 infection causes 80% of oral lesions. A majority of the population is infected by at least one herpes subtype of HSV-1 before adulthood. The infection in some cases does not produce any symptoms. Drugs for HSV-1 are becoming suppressive. In the present study, isolation of endophytic bacteria was carried out from medicinal plant. A grown bacterium was identified and confirmed using molecular 16S rRNA sequencing followed by extraction of bioactive compounds using solvents. Twelve bioactive compounds were then investigated for in vitro cytotoxicity assay and in vitro antiviral assay. Chloroform extract was found to be effective in inhibiting the virus.

126-133

Authors: S. G. Dhage, G. K. Lohiya, Y. M. Charde*, J. G. Avari

Certain problems regarding the drugs like high first pass metabolism, also the bioavailability of the certain drugs varies due to instability in acidic environment of stomach. Hence, to resolve such problems the drug should be incorporated in the microspheres for sustained release using a suitable polymer. Natural polymer like chitosan gained great interest in pharmaceutical sector because of its advantages like biodegradability, biocompatibility, non-toxicity, non-immunogenicity and low cost. In the present study, formulation and evaluation of polymeric microspheres of Atorvastatin Calcium was carried out and the release profile of such drug using the alginate and chitosan was studied. Microspheres were prepared for sustained release of drug using chitosan and alginate polymers by ionotropic gelation method. Microspheres were spherical in shape, having good flow properties and further its encapsulation efficiency, swelling index, micromeritic study, in- vitro drug release study and stability studies were performed in order to characterize microspheres. Three different concentrations of sodium alginate (1%, 2% and 3%) were used. The higher encapsulation efficiency was observed as the concentration of alginate increased. This is due to the greater availability of active calcium binding sites in the polymeric chains and consequently the greater degree of cross linking. The highest encapsulation efficiency (88.36) was achieved with 2% w/v sodium alginate in combination with 3% chitosan (F6). Among the prepared formulations with respect to the entrapment efficiency, swelling studies and in vitro drug release, the alginate-chitosan microspheres prepared by ionotropic gelation using calcium chloride found to be better than ionically cross linked alginate spheres alone. Therefore, dual cross-linked, microspheres are promising carrier for sustained release of drug.

139-144

Authors: Debarshi Kar Mahapatra1*, Devashish Das2, Ruchi Shivhare3

Cancer is the second leading causes of mortality across the planet which has had affected millions. In spite of massive efforts in producing new molecules and chemotherapeutic approaches for managing cancer, it continued to be the global threat. Small hybrid molecules have gained popularity in chemotherapy due to their potential and smart characteristics in modulating biological targets. The present research attempts in developing few novel hybridized derivatives of murrayanine (an active carbazole derivative) by the semi-synthetic approach to form substituted thiazole linked murrayanine-Schiff’s base derivatives. The protocol involved murrayanine 1 as the template material for constructing a hybridized Schiff’s base intermediate 3, which further by Hantzch’s cyclization was subsequently converted to various hybridized thiazoles analogs 5a-5f. The purity of the synthesized compounds was ascertained by sophisticated analytical techniques. The anti-cancer potential was screened against breast cancer cell lines; MCF-7 and MDA-MB-231 by Sulforhodamine B (SRB) assay. The compound 5b displayed most potent anti-proliferative activity with IC50 values of 23.41μM against MCF-7 cell line and 32.15μM against MDA-MB-231 cell line. It has been observed that analogs having electron withdrawing substituents exhibited pronounced anticancer activity. The docking study was performed by Autodock Vina where the results were found to be in full agreement with the cytotoxic study, depicting that the probable cytotoxic outcome by EGFR inhibitory mechanism. The study revealed the potential of novel hybridized derivatives as active anti-breast cancer candidates. The research will encourage (medicinal) chemists in rationally designing of semi-synthetic analogs of a heterocyclic prototype having pronounced anti-cancer activity.