Formulation and Optimization of Mucoadhesive Nanodrug Delivery System of Acyclovir

Formulation and Optimization of Mucoadhesive Nanodrug Delivery System of Acyclovir

Pharmaceutics Formulation and Optimization of Mucoadhesive Nanodrug Delivery System of Acyclovir Bhosale UV, Kusum Devi V, Jain N Department of Pharm...

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Pharmaceutics

Formulation and Optimization of Mucoadhesive Nanodrug Delivery System of Acyclovir Bhosale UV, Kusum Devi V, Jain N Department of Pharmaceutics, Al-Ameen College of Pharmacy, Bangalore - 560 027, India Address for correspondence: Mr. Uday Bhosale; E-mail: [email protected]

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INTRODUCTION

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Journal of Young Pharmacists Vol 3 / No 4

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Bhosale, et al.: Mucoadhesive nano drug delivery system of acyclovir

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In vitro characterization of PLGA nanoparticles Journal of Young Pharmacists Vol 3 / No 4

Bhosale, et al.: Mucoadhesive nano drug delivery system of acyclovir Table 1: ([perimental GesiJn anG parameters for 23 fXll factorial GesiJn batcKes Batch code MF1 MF2 MF3 MF MF MF MF MF C

Variable level in Particle % Drug % Drug Average % coded form size entrapment release intestinal (nm) in 12 h retention X3§ X1* X2# +1 +1 +1 1 93  93 í1 +1í1 +1 121 99 92 21 +1 í1 +1 13 91 332  í1 +1 +1 12 12 3  +1 +1 í1  12 33 2 í1 í1 í1  1 11 3 +1 í1 í1 91 2 32 2 í1 í í1 1 9 2 9 í í 11 9 3 -

For PL*A  ;1 transIormed levels in polymer weight are í1 = 1 mg +1 = 2 mg í = 193 mg #For surIactant pluronic F ;2 transIormed levels in  are í1 = 2 +1 = 3 í = 22 §For mucoadhesive polymer polycarbophil ;3 transIormed levels in  are í1 = 1 +1 = 1 í = 112

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Bhosale, et al.: Mucoadhesive nano drug delivery system of acyclovir

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b Figure 1: SEM of PLGA nanoparticles Journal of Young Pharmacists Vol 3 / No 4

Figure 3: Comparison of % drug entrapment and % drug release in JQHHCEVQTKCNCPFEJGEMRQKPVHQTOWNCVKQPU 279

Bhosale, et al.: Mucoadhesive nano drug delivery system of acyclovir

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hosale et al.: Mucoadhesive nano drug delivery system of acyclovir

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Figure 4: Average % drug release of mucoadhesive factorial formulations

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Formulation

Predicted values Observed values Particle % Drug % Particle % Drug % size entrapment Drug size entrapment Drug (nm) release (nm) release in 12 h in 12 h 112 31 3 11 9 3

7KH UHVSRnVH VXUIaFH SORWV and FRnWRXU SORWV iOOXVWUaWH WKaW aV WKH FRnFHnWUaWiRn RI SRO\PHUV 3/*A and SRO\FaUERSKiO inFUHaVHV WKH YaOXH RI dHSHndHnW YaUiaEOH iH SaUWiFOH Vi]H inFUHaVHV aOVR aV WKH FRnFHnWUaWiRn RI VWaEiOi]HU SOXURniF ) inFUHaVHV WKH YaOXH RI dHSHndHnW YaUiaEOH iH SaUWiFOH Vi]H dHFUHaVHV 6iPiOaUO\ WKH UHVSRnVH VXUIaFH SORWV and FRnWRXU SORWV IRU  dUXJ HnWUaSPHnW VKRZV SRViWiYH HIIHFWV RI indHSHndHnW YaUiaEOH iH SRO\PHU FRnFHnWUaWiRnV 3/*A and SRO\FaUERSKiO and nHJaWiYH HIIHFW RI RWKHU indHSHndHnW YaUiaEOH iH FRnFHnWUaWiRn RI VWaEiOi]HU SOXURniF )  BXW in FRnWUaVW WR WKiV iOOXVWUaWiRn WKH UHVSRnVH VXUIaFH SORW and FRnWRXU SORW IRU  dUXJ UHOHaVH in  K VKRZV nHJaWiYH HIIHFW RI indHSHndHnW YaUiaEOH iH SRO\PHU FRnFHnWUaWiRnV 3/*A and SRO\FaUERSKiO and SRViWiYH HIIHFW RI indHSHndHnW YaUiaEOH iH FRnFHnWUaWiRn RI VWaEiOi]HU SOXURniF ) Rn  dUXJ UHOHaVH in  K 0XFRadKHViRn inYROYHV diIIHUHnW NindV RI inWHUaFWiRn IRUFHV EHWZHHn PXFRadKHViYH PaWHUiaOV and PXFXV VXUIaFH VXFK aV HOHFWURVWaWiF aWWUaFWiRn K\dURJHn ERndinJ 9an dHU :aaOV IRUFHV and PHFKaniFaO inWHUSHnHWUaWiRn and HnWanJOHPHnW>@ 6SHFWURSKRWRPHWUiF PHWKRd OPa[  nP XVHd WR PHaVXUH in vitro PXFRadKHViYH FaSaFiW\ RI dHYHORSHd IRUPXOaWiRnV VKRZV WKH  inWHVWinaO UHWHnWiRn RI PXFRadKHViYH nanRSaUWiFOHV in WKH UaW inWHVWinaO PXFRVa 7KH adKHViRn SURSHUWiHV RI nanRSaUWiFOHV inFUHaVHd ZiWK inFUHaVinJ FRnFHnWUaWiRn RI PXFRadKHViYH SRO\PHU SRO\FaUERSKiO  281

Bhosale, et al.: Mucoadhesive nano drug delivery system of acyclovir

aPRnJ WKH YaUiRXV FRnFHnWUaWiRnV RI SRO\FaUERSKiO EHWWHU PXFRadKHViRn ZaV REVHUYHd IRU 0) and 0) IRUPXOaWiRnV aV 3 and  UHVSHFWiYHO\ >7aEOH @ '6& JiYHV inIRUPaWiRn UHJaUdinJ WKH SK\ViFaO SURSHUWiHV OiNH FU\VWaOOinH RU aPRUSKRXV naWXUH RI WKH VaPSOHV 7KH '6& WKHUPRJUaP RI aF\FORYiU >)iJXUH a@ VKRZV an H[RWKHUPiF SHaN aW 3 FRUUHVSRndinJ WR iWV PHOWinJ WHPSHUaWXUH ZKiFK ZaV nRW dHWHFWHd in WKH WKHUPRJUaPV IRU aF\FORYiUORadHd FRaWHd and XnFRaWHd nanRSaUWiFOHV RI 3/*A  >)iJXUHV E and F@ ,W KaV EHHn VKRZn E\ a FRXSOH RI aXWKRUV WKaW ZKHn WKH dUXJ dRHV nRW VKRZ iWV H[RWKHUPiF SHaN in WKH IRUPHd nanRSaUWiFOHV iW iV Vaid WR EH in WKH aPRUSKRXV VWaWH>@ +HnFH iW FRXOd EH FRnFOXdHd WKaW in ERWK WKH SUHSaUHd 3/*A nanRSaUWiFOHV FRaWHd and XnFRaWHd  WKH dUXJ ZaV SUHVHnW in WKH aPRUSKRXV SKaVH and Pa\ KaYH EHHn KRPRJHnHRXVO\ diVSHUVHd in WKH 3/*A PaWUi[

CONCLUSION

3/*A nanRSaUWiFOHV ZHUH SUHSaUHd E\ WKH VROYHnW dH SRViWiRn PHWKRd and ZHUH FKaUaFWHUi]Hd aV ´PXFRadKHViYHµ E\ FRaWinJ ZiWK PXFRadKHViYH SRO\PHU SRO\aFU\OiF aFid SRO\FaUERSKiO  7KH aSSOiFaWiRn RI IaFWRUiaO dHViJn JaYH a VWaWiVWiFaOO\ V\VWHPaWiF aSSURaFK IRU WKH IRUPXOaWiRn RI nanRSaUWiFOHV ZiWK WKH dHViUHd SaUWiFOH Vi]H KiJK HnWUaSPHnW HIÀFiHnF\ and VXVWainHd dUXJ UHOHaVH 'UXJ SRO\PHU UaWiR and FRnFHnWUaWiRn RI VXUIaFWanW ZHUH IRXnd WR inIOXHnFH WKH SaUWiFOH Vi]H and  dUXJ UHOHaVH RI aF\FORYiUORadHd 3/*A PXFRadKHViYH nanRSaUWiFOHV In vitro dUXJ UHOHaVH VWXd\ RI aOO IRUPXOaWiRnV 0)²0) VKRZHd ²3 dUXJ UHOHaVH in 3 K 7KH UHOHaVH ZaV IRXnd WR IROORZ )iFNian aV ZHOO aV nRn)iFNian diIIXViRn PHFKaniVP ZiWK aOPRVW ]HURRUdHU dUXJ UHOHaVH IRU aOO EaWFKHV In vitro inWHVWinaO PXFRadKHViRn RI nanRSaUWiFOHV VKRZHd WKaW WKH adKHViRn SURSHUWiHV RI nanRSaUWiFOHV inFUHaVHd ZiWK inFUHaVinJ FRnFHnWUaWiRn RI PXFRadKHViYH SRO\PHU SRO\FaUERSKiO  7KHVH SUHOiPinaU\ UHVXOWV indiFaWH WKaW aF\FORYiUORadHd PXFRadKHViYH 3/*A nanRSaUWiFOHV FRXOd EH HIIHFWiYH in VXVWaininJ dUXJ UHOHaVH IRU a SURORnJHd SHUiRd )XUWKHU VWXdiHV aUH nHHdHd WR FRnÀUP iWV SHUIRUPanFH in vivo 7KXV WKH aERYH inYHVWiJaWiRn inYROYHV H[WHnViYH and indHSWK KROiVWiF VWXdiHV RI PXFRadKHViYH and ViWHVSHFiÀF

Figure 5: Response surface plots of effects of factorial variables on % drug entrapment

Figure 6: Response surface plots of effects of factorial variables on particle size

Figure 7: Response surface plots of effects of factorial variables on % drug release in 12 h 282

Figure 8: DSC thermograms Journal of Young Pharmacists Vol 3 / No 4

hosale et al.: Mucoadhesive nano drug delivery system of acyclovir

nanRSaUWiFOHV WaiORUHd WR aFKiHYH FRnWUROOHd UHOHaVH RI SUHdHWHUPinHd TXanWiWiHV RI WKH dUXJ UHVXOWinJ in nRW RnO\ RSWiPi]inJ dUXJ dHOiYHU\ EXW aOVR dHYHORSPHnW RI a SOaWIRUP WHFKnRORJ\ ZKiFK KaV H[WHnViYH SaWHnWinJ SRWHnWiaO and Fan EH XVHIXO IRU VR Pan\ RWKHU VXFK dUXJV REFERENCES 

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Author Query Q1: Please define legends???

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Journal of Young Pharmacists Vol 3 / No 4

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