Formulation and Evaluation of Mucoadhesive Microspheres of an Anti-Hypertensive Drug

“ FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-HYPERTENSIVE DRUG. ”

SYNOPSIS FOR

M.PHARM DISSERTATION

SUBMITTED TO

RAJIVGANDHIUNIVERSITY OF HEALTH SCIENCES

KARNATAKA

GOWTHAM.M

I st M.PHARM

DEPARTMENT OF PHARMACEUTICS

PESCOLLEGE OF PHARMACY

HANUMANTHNAGAR

BANGALORE-560050

(2008-09)

RAJIVGANDHIUNIVERSITY OF HEALTH SCIENCES,

KARNATAKA, BANGALORE.

ANNEXURE-II

PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION

1 Name of the Candidate and Address:-

/ GOWTHAM.M
P.E.S.COLLEGE OF PHARMACY
50, FEET ROAD
HANUMANTH NAGAR
BANGALORE-560050.
PERMANENT ADDRESS
s/o.A.VENUGOPALAN.
‘SREE’,NEAR PAYYANURCOLLEGE
EDAT-670327
KANNUR(DT)
KERALA.
2 / Name of the Institution:- /

P.E.S.COLLEGE OF PHARMACY

50 FEET ROAD
HANUMANTH NAGAR
BANGALORE-560050.
3 / Course of Study and Subject:- /

MASTER OF PHARMACY IN PHARMACEUTICS

4 / Date of the Admission :- / 1st June 2008.
5 /

Title of the topic:-

“FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-HYPERTENSIVE DRUG. ”
6 / Brief resume of the intended work:
6.1 Need for the study:-
Hypertension is a medical condition in which blood pressure is chronically elevated, ie BP is >=140/90mmHg.
If not,effectively treated it may lead to strokes, myocardial infarction,
Retinopathy,Nephropathy etc.
Anti hypertensives are the class of drugs that are used to treathypertension. Evidences suggest that reduction in BP by 5-6 mmHg decreases the risk of stroke by 40%, coronary heart disease by 15-20% and reduces heart failure,nephropathy etc
For treatment of hypertension a sustained release of medicament is needed to achieve a steady state plasma concentration for longer period.Conventional therapy requires frequent administration which reduces patient compliance and requires high concentration to maintain the therapeutic effect.
Microspheres based drug delivery system has received a wide appreciation due to its flexibility,cost effectiveness and broad regulatory acceptance.
Among microspheres Mucoadhesive Microspheres have many advantages like-

Efficient absorption.
Enhanced bioavailability.
Prolonged gastro intestinal time.
High surface to volume ratio which ensures a much more intimate contact with mucus layer
Specific targeting of drugs to absorption site.
Better control of systemic drug delivery etc..

A lot of work has been carried out to maintain the sustained effect of the therapeutic agents by preparing the microspheres and they have been found to be very effective delivery system.
6.2 Review of the literature:-
Harikarnpakdee S et al. made spray dried mucoadhesive microspheres of Propranolol Hydrochloride using various polymers.It was found that Chitosan showed maximum adhesion than Carbopol 934P.(1)
 Paharia Aet al. made Eudragit coated pectin microspheres of 5-Fluro Uracil for colon targeting.They were prepared by emulsion dehydration method using different drug: polymer ratios, stirring speed and emulsifier concentration.(2)
Dandagi PM et al . made mucoadhesive microspheres of Propranolol Hydrochloride for nasal delivery. It was observed that all microspheres showed good bioadhesive properties, swelling indices and good sustain release of drug.(3)
Kilicarslan M and Baykara T studied the effect of drug/polymer ratio on properties of Verapamil Hydrochloride loaded microspheres using solvent evaporation method.It was found that the variation in drug/polymer ratios have an influence on the physical characteristics of microspheres and increase in amount of polymer results in decrease in drug release.(4)
SahooSK et al . formulated and evaluated eudragit microspheres of Stavudine by solvent evaporationmethod.The microspheres showed good drug entrapment and drug release was extended.(5)
Halder A and Biswanath S prepared and evaluated Polystyrene coated Diltiazem Hydrochloride resin complex by O/W emulsion solvent evaporation method.It was found that both encapsulation efficiency and drug release was influenced by uniformity of coating and formulation parameters.(6)
Patel JK et al .formulated and evaluated mucoadhesive microspheres of Glipizide using simple emulsification phase separation method.The drug release was sustained for longer time and percentage of mucoadhesion was good.(7)
Bahar BH et al . studied the influence of aluminium tristearate and sucrose as dispersing agents on physical properties and release characteristics of Verapamil Hydrochloride – Eudragit Rs microspheres.It was concluded that concentration of dispersing agents effected the physical properties and drug release from microsppheres.(8)
Jain Det al . developed Eudragit S 100 entrapped Insulin microspheres.It was observed that the microspheres protected Insulin from proteolytic degradation in GIT.(9)
Kim BK et al . prepared and characterized drug loaded polymethacrylate microspheres by emulsion solvent evaporation method using Felodipine as the drug.The release rate of Felodipine from polymers was found to be controlled by the choice of polymer type.(10)

6.3 Main objectives of the study:-
The objective of the present study is as follows :-
a)To formulate microspheres consisting of a model Anti Hypertensive drug.
b)To evaluate the microspheres for entrapment efficacy and dissolution studies.
c)To study the effect of polymers and polymer concentration on the drug release profile.
d)To carry out the stability studies on the selected formulations

7

/ Materials and methods:-
7.1 Source of data
The data will be obtained from experimental work, which includes
a) Formulation of the microspheres.
b)In vitroevaluation of the formulations.
c) Stability studies of the selected formulations.
7.2 Method of collection of data (including sampling procedures if any)
The data will be collected from prepared formulations subjected to different evaluation techniques, estimation of drug content, in-vitro drug release and stability studies.
7.3 Does the study require any investigation or interventions to be
Conducted on patients or other humans or animals?
No
7.4 Has ethical clearance been obtained from your institution in case of
7.3?
Not Applicable

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List of References:-

1.Harikarnpakdee S, Lipipun V, Sutanthavibul N , Ritthidej G . Spray-dried Mucoadhesive Microspheres: Preparation and Transport Through Nasal Cell Monolayer. AAPS PharmSciTech. 2006;7(1):E1-E10.
2.Paharia A, Yadav AK, Rai G, Jain SK, Pancholi SS, Agarwal GP. Eudragit-coated Pectin Microspheres of 5-Fluorouracil for Colon Targeting. AAPS PharmSciTech. 2007;8(1):E1-E7.
3.Dandagi PM, Mastiholimith VS, Gadad AP, Iliger SR . Mucoadhesive Microspheres of Propranolol Hydrochloride for Nasal Delivery.Int J Pharm Sci. 2007;69(3):402-7.
4.Kilicarslan M, Baykara T . The effect of the drug/polymer ratio on the properties of the Verapamil HCl loaded microspheres. Int J Pharm. 2003;252:99-109.
5.Sahoo SK, Mallick AA, Barik BB, Senapati PC. Formulation and in vitro Evaluation of Eudragit Microspheres of Stavudine. Trop J Pharm Res. 2005;4(1):369-75.
6.Halder A, Biswanath S. Preparation and In Vitro Evaluation of Polystyrene-Coated Diltiazem-Resin Complex by Oil-in-Water Emulsion Solvent Evaporation Method. AAPS PharmSciTech. 2006;7(2):E1-E8.
7.Patel JK, Patel RP, Amin AF, Patel MM. Formulation and Evaluation of Mucoadhesive Glipizide Microspheres. AAPS PharmSciTech. 2005;6(1):E49-E55.
8.Bahar BH, Kilicarslan M, Yuksel N, Baykara T. Influence of Aluminum Tristearate and Sucrose Stearate as the Dispersing Agents on Physical Properties and Release Characteristics of Eudragit RS Microspheres. AAPS PharmSciTech. 2006;7(1):E1-E7.
9.Jain D, Panda AK, Majumdar DK. Eudragit S100 Entrapped Insulin Microspheres for Oral Delivery. AAPS PharmSciTech. 2005;6(1):E100-E6.
10.Kim BK, Hwang SJ, Park JB, Park HJ. Preparation and characterization of drug-loaded polymethacrylate microspheres by an emulsion solvent evaporation method. J microencapsulation. 2002;19(6):811-22.