Volume 10, Issue 3, Jul-Sep 2018

Volume 10

July-September 2018

Drug delivery and therapeutic ‎approaches to prostate cancer

Jameel Ahmed S ‎Mulla

Abstract:
According to the global cancer statistics, prostate cancer is the second most often diagnosed cancer in males worldwide and it ranks in fifth place among cancerrelated deaths. Localized prostate cancer is usually treated by surgical removal of the prostate (radical prostatectomy) or by radiation therapy. Both treatment options are frequently associated with severe side effects. Drug delivery to prostate through conventional route is associated with pharmacokinetics based and side effects related problems. This review briefly highlighted about prostate structure and its cancer. Different therapeutic approaches such as radiotherapy, chemotherapy, immunotherapy, androgen deprivation therapy (ADT), focal therapies and systemic therapies; and drug delivery approaches such as liposomes, polymeric based nanoparticles and micelles, dendrimers, gold nanoparticles, carbon based nanoparticles and magnetic nanoparticles for prostate cancer are also outlined here.

Keywords: Prostate Structure, Prostate Cancer, Therapeutic Approaches, Drug Delivery Approaches, Liposomes, Nanoparticles.

Preparation and characterization of ‎marigolds (Cosmos caudatus L.) ‎Leaf extract-loaded nanoemulsion: ‎Physicochemical properties and in-‎vitro release activities of ‎nanoemulsion system using virgin ‎coconut oil (VCO)‎

Rahmi Annisa, ‎Roihatul Muti’ah, ‎Siti Maimunah, ‎Begum Fauziyah, ‎Zahratunnahdhati ‎Li’ibaadatillaah

Abstract:
Marigolds (Cosmos caudatus L.) leaves widely consumed as a vegetable and empirically been used as a medicine for various diseases. In this study, nanoemulsion was prepared using leaf extract of C. caudatus with a concentration of 5%, 10%, 15% and using Virgin Coconut Oil (VCO) as an oil phase. The purpose of this study is to know the characteristics of the formulation and to determine the effect of extract concentration on the release rate of the active compound of quercetin of C. caudatus leaf extract on the preparation. C. caudatus extract was obtained by the ultrasonic method with 96% methanol solvent. Nanoemulsion extracts were made by a low energy method. All formulations were evaluated for the preparation characteristics which included organoleptic test, pH test, particle size, emulsion type, entrapment efficiency, and stability, and quercetin release test of C. caudatus leaf extract using Franz cell diffusion method with cellophane membrane. The result of the characteristic evaluation of the research shows that formulation 1, 2, and 3 give a good result that is in accordance with the standard specification of each specified. The quercetin release flux of each nanoemulsion preparation formulation was 13,374 ± 0.216 μg / cm² / min, 9,617 ± 0.404 μg / cm² / min and 8,635 ± 0.021 μg / cm² / min respectively. This result shows that the higher of extract concentration, the longer the release time.

Keywords: Marigolds (Cosmos caudatus L.) leaf, Quercetin, Nanoemulsion, Extract Concentration, Release.

Simultaneous estimation of ‎curcumin and gefitinib in bulk, ‎plasma and brain homogenate by ‎RP-HPLC technique

Sagar Kishor Savale

Abstract:
The present study was aimed at developing a reversed phase high performance liquid chromatography (RP-HPLC) method for simultaneously determination of curcumin (CRM) and gefitinib (GFT) in bulk, plasma and brain homogenate and hydrochlorothiazide was used as an internal standard. A new simple, rapid, selective, precise and accurate reverse phase high performance liquid chromatography method has been developed. The separation was achieved by using C-18 column (Qualisil BDS C18, 250 mm x 4.6 mm I.D.) coupled with a guard column of silica, mobile phase was consisting of acetonitrile: water with 1% formic acid (30:70 v/v). The flow rate was 0.2 ml/min and the drug was detected using PDA detector at the wavelength of 242 nm. The experimental conditions, including the diluting solvent, mobile phase composition, column saturation and flow rate, were optimised to provide high-resolution and reproducible peaks. The method was developed and tested for linearity range of 10-60 μg/mL for bulk analysis and 200-800 ng/mL for plasma and brain homogenate. The method was validated as per ICH guidelines, the developed method was validated in terms of linearity, application of the proposed method to bulk sample, recovery, precision, repeatability, ruggedness, sensitivity (LOD and LOQ) and robustness, stability study (short and long-term stabilities, Freeze/thaw stability, post-preparative).The low value of % RSD showed that the method was precise within the acceptance limit of 2%. The developed method was successfully applied for the analysis of the drug in bulk as well as various marketed formulation and drug in plasma and brain distribution studies.

Keywords: RP-HPLC, Simultaneous Estimation, Plasma, Brain Homogenate, Curcumin, Gefitinib.

Development and characterisation ‎of donepezil nanoparticles

P V Kamala Kumari, ‎Y Srinivasa Rao, A ‎Naga Raju

Abstract:
The purpose of the present study was to formulate and evaluate donepezil loaded nanoparticles for effective treatment of Alzheimer’s disease. Nanoparticles were prepared by ionic gelation of chitosan with poloxamer. Size and morphology of nanoparticles were investigated. Scanning electron microscopy (SEM) revealed that the donepezil nanoparticles were smooth and spherical without any aggregation. F6 formulation which had drug polymer ratio of chitosan and poloxamer was decided to be the optimized formulation based on in vitro drug release studies. Dissolution data based on two different methods was fitted in zero order, first order and Higuchi equations. The mechanism of drug release was determined by using Higuchi equation. There was no significant change in physical and chemical properties of formulation F-6 even after three months.

Keywords: Nanoparticle, Diffusion Study, Donepezil, Higuchi, Stability Study.

In vitro characterization of ‎ethodolac gastro retentive hollow ‎microballons

M Swetha, B Rama‎‎, B Mohan, D ‎Muthulakshmi, ‎Aparna Peri

Abstract:
Etodolac has been used for treatment of Rheumatoid Arthritis(RA) and Osteoarthritis. It is a BCS class II drug i.e. low solubility & high permeability and major absorption site is stomach region. It shows dissolution rate-dependent bioavailability. This work was carried out to improve the dissolution rate and controlled release of drug so it could retain in the stomach for longer period of time delivering to the site of action i.e. stomach. Aim of the present work is to prepare and characterization of Gastro Retentive Hallow Micro Balloons of etodolac by using two acid resistant polymers such as Eudragit RS 100 & ethyl cellulose with different ratio, Eudragit RS 100 is water insoluble over the entire range of pH it swells in stomach in swollen state it is permeable to water and dissolved actives. In this study solvent diffusion /evaporation technique was used to prepare a gastro retentive hallow micro balloons for etodolac and influence of several factors on various physical characteristics, including particle size, buoyancy, drug entrapment /loading, in vitro dissolution drug release characters are investigated.

Keywords: Ethodolac, RA, Osteoarthritis, BCS II, Eudragit RS 100, Buoyancy, Drug Entrapment.

Indian Journal of

Novel Drug Delivery ISSN 0975-5500

Indian Journal of Novel Drug Delivery ISSN 0975-5500