Review Article

Receptor based treatment: A solution to clinical problems in HIV/AIDS

Rajat Batra*, Shruti Rayan

SVKM’S Narsee Monjee Institute of Management Studies, School of Pharmacy and Technology Management, Mumbai-Agra Road, Shirpur, India.

*Corresponding Author: Tel.: +91 7709946364; E-mail address: rajat.sptm.2019@gmail.com

One of the most fatal and epidemic disease, Acquired Immunodeficiency Syndrome (AIDS) since the past century has shown its adverse effects on the society all over the globe. The current population of people suffering from AIDS/HIV is about 36.6 million. During years of research on human immunodeficiency virus (HIV), we have gathered a lot of information on its receptor cells which were studied as CCR5 along with CD4 and CXCR4. These studies have enlightened our knowledge about Acquired immunodeficiency syndrome (AIDS) and its pathogenesis. The study of the receptors and its interaction with the glycoproteinaceous envelope of HIV led to anti-retroviral drugs therapy based on blocking the fusion or docking of virus to the host cell. CCR5 receptor polymorphism helps us to determine its resistance to the HIV infection.

Keywords: AIDS, CXCR4, CCR5, HIV, CD4, Receptors, Cell receptors

Original Article

Estimation of Amlodipine in human plasma by liquid chromatography tandem mass spectrometry

Rajeev K. Gupta^a,*, Anand Chaurasia^b, Brijesh K. Mishra^c, Vibha Chaturvedi^d, Pratik K. Gupta^d

^aDepartment of Pharmaceutical Sciences, MJRP University, Jaipur, India.

^bDepartment of Pharmacy, RKDF University, Bhopal, India.

^cSchool of Pharmacy, RGPV, Bhopal, India.

^dMewar University, Chittorgarh Rajasthan, India.

*Corresponding Author: Tel.: +91 8126407501; Email address: rkpipraiya@gmail.com

A simple, accurate, precise and cost effective bioanalytical method was developed and validated in human plasma by high performance liquid chromatography/positive ion electro spray tandem mass spectrometry. Liquid liquid extraction with ethyl acetate was used for extraction of the drug from plasma and the analytes were separated using isocratic mode on a reversed- phase column Hypurity C18 50X 2.1 mm, 5µ and analyzed by mass spectrometry in the multiple reaction monitoring mode using the respective [M+H] Ions, m/z was 409.2/238.0 for Amlodipine along with m/z 406.3.2/151.1 for Nebivolol as internal standard. The method exhibited a linear dynamic range between 0.10 to 20.12 ng/mL concentrations for Amlodipine in human plasma. Method development and full method validation was performed along with all stability parameter. The validated method can be used to analyze human plasma samples for its pharmacokinetics application, bioavailability and bioequivalence studies.

Keywords: Stability, Nebivolol, Amlodipine, Human Plasma, Validation, Bioanalytical

Original Article

Development and characterization of ethosomes based gel formulation for enhanced topical delivery

Anupam K. Sachan, Ankita Gupta *, Pratibha Gupta

Dayanand Dinanath College, Institute of Pharmacy, Kanpur, India.

*Corresponding Author: Tel.: +91 9889519511; E-mail address : gupta.ankita483@gmail.com

The present research work aims at development and evaluation of diclofenac loaded ethosomal gel. The innumerable adverse effects due to oral use of diclofenac impelled to develop topical drug loaded ethosomal gel for better patient compliance and reduced adverse effects. The ethosomes were prepared by hot method using different ratios of polymers, ethanol and propylene glycol. The prepared ethosomes were characterized by morphological studies, entrapment efficiency and zeta potential. The vesicle size and entrapment efficiency varied from 180 to 930 nm and 38% to 90% respectively. The gel was prepared by incorporating ethosomal dispersions containing drug into the Carbopol gel under mechanical stirring. Gel formulations were characterized for pH determination, spreadability, drug content, viscosity measurement, and in vitro drug diffusion studies. FT-IR and stability studies of the prepared formulation were also investigated. FT-IR studies confirmed that there was no chemical interaction between drug and excipients used in the formulation. Formulation F8 with maximum drug content of 9.98 % and drug release of 82.13 % was selected as best formulation. From this research work it can be deduced that topical ethosomal gel formulation is a promising system for excellent percutaneous absorption of drug.

Keywords: Diclofenac, Carbopol 940, Propylene Glycol, Ethosomes

Original Article

Comparative study of lactogenic activity reported on ethanolic extract of Basella Alba (Linn) leaf and root on lactating albino wistar rats

Sangeeta Gupta*

Department of Pharmacognosy, Moradabad Educational Trust, Group of Institution, Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

*Corresponding Author: Tel.: +91 9627953280; E-mail address: nicesangi@gmail.com

In view of the traditional belief that the whole plant of Basella alba has been used to stimulate milk production in lactating women, experiments were performed to determine a comparative study on extract EBAR (Ethanolic Basella alba root) and EBAL(Ethanolic Basella alba leaves) on milk production in rats. Female lactating rats with suckling pups were orally administered with EBAL and EBAR extract and continued for l5th day of parturition. Milk yield, the body weight of pups and mother were measured daily. On 15th day, the total protein/glycogen contents from mammary tissue and serum prolactin/cortisol level from blood sample were measured and compared with control. Oral administration of EBAL and EBAR extract increases the milk yield, body weight of pups as well as mother rat. Along with glycogen and protein content as well as serum prolactin and cortisol level were also raised when compared to the control animal. In addition, the lactogenic effect of EBAL at dose (500 mg/kg, bw) was found to be higher as compared EBAR extract and control group. The present study revealed that the Basella alba leaf extract possesses significant lactogenic activity by enhancing milk production and prolactin concentration in nursing rats.

Keywords: Lactogenic activity, Milk production, Basella alba, Galactogouge activity

Original Article

An approach towards optimized dendrimer based delivery technology to modify drug loading and release of Vinorelbine

Satyaswarup Samantray^a,*, Sudhansu R. Swain^b, Shailesh Sharma^c

^aMylan Laboratories Ltd. R&D Center, Bollaram, Hyderabad, Andhra Pradesh, India.

^bMoradabad Educational Trust, Group of Institutions – Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

^cDepartment of Pharmaceutics, NIMS Institute of Pharmacy, NIMS University, Jaipur, Rajasthan, India.

*Corresponding Author: Tel.: +91 7702686117; E-mail address: pulin83@gmail.com

The antitumor activity of vinorelbine may be due to primarily inhibition of mitosis during metaphase and its interaction with tubulin. The aqueous solubility of the drug is > 1000 mg/mL in distilled water. Prolonged vinorelbine exposure is correlated with improved antineoplastic effects, as evidenced by increased response rate in patients receiving continuous infusion. A phase I pharmacokinetic study of the Vinorelbine liposomal injection has been reported and concluded well tolerated and exhibited more favorable pharmacokinetic profiles than free vinorelbine. Dendrimers are new class of artificial macromolecules. Dendrimers possess a well-defined topological structure, are versatile candidates as scaffolds or vehicles for nanomedicine in the field of cancer diagnosis and therapy. Dendrimers can be used for loading of anticancer compounds and by non-covalent interactions (ionic, hydrophobic, hydrogen-bond interactions), covalent bindings and spacer-mediated conjugates. Also, they can be used for targeting to cancer cells, tumour tissues, or abnormal vessels adjacent to the disease focus based on the molecular ‘‘hooks’’ conjugated on the surface of dendrimer through active targeting, and can be accumulated in tumours via the enhanced permeability and retention (EPR) effect of the nanosized dendrimer through passive targeting effect of the nanosized dendrimer through passive targeting. In this study we developed an optimized technology to conjugate Vinorelbine to PAMAM dendrimers for improved release and better stability than the liposomal delivery system.

Keywords: Vinorelbine, PAMAM dendrimer, Cancer, Drug delivery system

Original Article

Evaluation of learning and memory activity of poly-herbal formulation by scopolamine and stress induced amnesia

Kisalaya Mishra, Deepa, Hemant Nagar

Truba Institute of Pharmacy, Bhopal, Madhya Pradesh, India.

*Corresponding Author: Tel.: +91 7800020461; E-mail address: kisalayamishra@yahoo.in

Normal ageing is not as much as responsible for causing memory disorder as such, but it is associated with a general decline in cognitive and neural systems, including memory. As people age, the likelihood of cholinergic dysfunction, betaamyloid deposits, hippocampal neurofibrillary tangles or neurotic plaques in the cortex of the brain increases, so that memory connections can become blocked, memory functions decrease and the likelihood of memory disorders like dementia and Alzheimer’s disease increases. Ageing is the single greatest risk factor for neurodegenerative diseases in general. Recent research reveals some major consequences between cognitive changes of normal ageing and other neurodegenerative diseases known as mild cognitive impairment were some memory loss occurs which doesn’t interferes with normal daily functioning. More severe memory loss is defined as dementia; those patients who have mild cognitive impairment are at high risk of developing Alzheimer like diseases. Currently the commercial use of the synthetic cognitive enhancers shows some of its downs effects on the brain not only functionally but also have unexpected complications. That why the area of thirst is to explore such poly-herbal formulations with meets and fulfil the optimized level of therapeutic efficiency and efficacy without any side effects.

Keywords: β-amyloid, Hippocampal, Neurofibrillary tangles, Dementia, Alzheimer