Main Article Content
treatment of Parkinsonâ€™s disease, that will sustain drug release up to 1 month. Biodegradable microspheres of RPN were
prepared by using two different polymers (poly lactic co glycolic acid [PLGA] 50:50 and PLGA 75:25) employing double
emulsion (W/O/W) solvent evaporation method. Preliminary optimization of process parameter was done for concentration
of polyvinyl alcohol (PVA) solution, stirring speed, temperature of PVA solution, ratio of the drug to polymer (D/P) and
ratio of internal phase to external phase volume (IP/EP). All formulations were evaluated for particle size, percentage yield,
entrapment efficiency (EE), shape etc. Formulation E3 and E4 shows maximum EE. % in vitro drug release per day of E3 and
E4 batch was studied. The RPN was incorporated successfully in microspheres prepared with 0.5% w/v PVA at 8000 RPM
stirring speed, 20Â°C processing temperature, 1:4 drug polymer ratio and 1:30 IP/EP ratio, which provides sustained release
up to 4 weeks with better efficacy and patient compliance and can be employed as an alternative to existing oral medications.
Key words: Entrapment efficiency, poly lactic co glycolic acid 50:50, polyvinyl alcohol, solvent evaporation, sustained release
This is an Open Access article distributed under the terms of the Attribution-Noncommercial 4.0 International License [CC BY-NC 4.0], which requires that reusers give credit to the creator. It allows reusers to distribute, remix, adapt, and build upon the material in any medium or format, for noncommercial purposes only.
Chaudhuri RK, Martinez-Martin P, Rolfe KA, Cooper J, Rockett CB,
Giorgi L. Improvements in nocturnal symptoms with ropinirole
prolonged release in patients with advanced Parkinsonâ€™s disease. Eur
J Neurol 2012;19:105-13.
Eden RJ, Costall B, Domeney AM, Gerrard PA, Harvey CA, Kelly ME, et al.
Preclinical pharmacology of ropinirole (SK and F 101468â€‘A) a novel
dopamine D2 agonist. Pharmacol Biochem Behav 1991;38:147â€‘54.
Hatefi A, Amsden B. Biodegradable injectable in situ forming drug
delivery systems. J Control Release 2002;80:9â€‘28.
Berkland C, Kim K, Pack DW. Fabrication of PLG microspheres with
precisely controlled and monodisperse size distributions. J Control
Jain RA, Rhodes CT, Railkar AM, Malick AW, Shah NH. Controlled
release of drugs from injectable in situ formed biodegradable PLGA
microspheres: Effect of various formulation variables. Eur J Pharm
Sun Y, Wang J, Zhang X, Zhang Z, Zheng Y, Chen D, et al. Synchronic release
of two hormonal contraceptives for about one month from the PLGA
microspheres: In vitro and in vivo studies. J Control Release 2008;129:192â€‘9.
Jeffery H, Davis SS, Oâ€™Hagan DT. The preparation and characterization of
poly (lactideâ€‘coâ€‘glycolide) microparticles. II. The entrapment of a model
protein using a (waterâ€‘inâ€‘oil)â€‘inâ€‘water emulsion solvent evaporation
technique. Pharm Res 1993;10:362â€‘8.
Jiang W, Gupta RK, Deshpande MC, Schwendeman SP. Biodegradable
poly (lacticâ€‘coâ€‘glycolic acid) microparticles for injectable delivery of
vaccine antigens. Adv Drug Deliv Rev 2005;57:391â€‘410.
Gu H, Song C, Long D, Mei L, Sun H. Controlled release of recombinant
human nerve growth factor (rhNGF) from poly[(lactic acid)â€‘coâ€‘(glycolic
acid)] microspheres for the treatment of neurodegenerative disorders.
Polym Int 2007;56:1272â€‘80.
Conway BR, Oya AH. Double emulsion microencapsulation of proteins
as model antigens using polylactide polymers: effect of emulsifiers on
microsphere characteristics and release kinetics. Eur J Pharm Biopharm
Ogawa Y, Yamamoto M, Okada H, Yashiki T, Shimamoto T. A new
technique to efficiently entrap leuprolide acetate into microcapsules of
polylactic acid or copoly (lactic/glycolic) acid. Chem Pharm Bull (Tokyo)
Aubertâ€‘PouÃ«ssel A, Venierâ€‘Julienne MC, Clavreul A, Sergent M,
Jollivet C, Monteroâ€‘Menei CN, et al. In vitro study of GDNF release from
biodegradable PLGA microspheres. J Control Release 2004;95:463â€‘75.
Prior S, Gamazo C, Irache JM, Merkle HP, Gander B. Gentamicin
encapsulation in PLA/PLGA microspheres in view of treating Brucella
infections. Int J Pharm 2000;196:115â€‘25.
Zolnik BS, Burgess DJ. Evaluation of in vivoâ€‘in vitro release of
dexamethasone from PLGA microspheres. J Control Release
Arshady R. Preparation of biodegradable microspheres and
microcapsules: Polylactides and related polyesters. J Control Release
Parikh RH, Parikh JR, Dubey RR, Soni HN, Kapadia KN. Poly (D,
Lâ€‘lactideâ€‘coâ€‘glycolide) microspheres containing 5â€‘fluorouracil:
Optimization of process parameters. AAPS Pharm Sci Tech 2003;4:E13.
Lee SC, Oh JT, Jang MH, Chung SI. Quantitative analysis of polyvinyl
alcohol on the surface of poly (D, Lâ€‘lactideâ€‘coâ€‘glycolide) microparticles
prepared by solvent evaporation method: Effect of particle size and
PVA concentration. J Control Release 1999;59:123â€‘32.
Yang YY, Chung TS, Bai XL, Chan WK. Effect of preparation conditions
on morphology and release profiles of biodegradable polymeric
microspheres containing protein fabricated by doubleâ€‘emulsion
method. Chem Eng Sci 2000;55:2223â€‘36.
Lu L, Peter SJ, Lyman MD, Lai HL, Leite SM, Tamada JA, et al. In vitro and
in vivo degradation of porous poly (DLâ€‘lacticâ€‘coâ€‘glycolic acid) foams.
Park TG. Degradation of poly (lacticâ€‘coâ€‘glycolic acid) microspheres:
Effect of copolymer composition. Biomaterials 1995;16:1123â€‘30.
Makadia HK, Siegel SJ. Poly lacticâ€‘coâ€‘glycolic acid (PLGA) as
biodegradable controlled drug delivery carrier. Polymers (Basel)