Abstract
This work is the continuation of a study focused on establishing relations between surface thermodynamic properties and in vitro release mechanisms using a model drug (ampicillin trihydrate), besides analyzing the granulometric properties of new polymeric materials and thus establishing the potential to be used in the pharmaceutical field as modified delivery excipients. To do this, we used copolymeric materials derived from maleic anhydride with decreasing polarity corresponding to poly(isobutylene-alt-maleic acid) (hydrophilic), sodium salt of poly(maleic acid-alt-octadecene) (amphiphilic), poly(maleic anhydride-alt-octadecene) (hydrophobic) and the reference polymer hydroxyl-propyl-methyl-cellulose (HPMC). Each material alone and in blends underwent spectroscopic characterization by FTIR, thermal characterization by DSC and granulometric characterization using flow and compaction tests. Each tablet was prepared at different polymer ratios of 0%, 10%, 20%, 30% and 40%, and the surface properties were determined, including the roughness by micro-visualization, contact angle and water absorption rate by the sessile drop method and obtaining Wadh and surface free energy (SFE) using the semi-empirical models of Young–Dupré and Owens-Wendt-Rabel-Käelbe (OWRK), respectively. Dissolution profiles were determined simulating physiological conditions in vitro, where the kinetic models of order-zero, order-one, Higuchi and Korsmeyer–Peppas were evaluated. The results showed a strong relationship between the proportion and nature of the polymer to the surface thermodynamic properties and kinetic release mechanism.
Highlights
The development of new devices for controlled release of drugs corresponds to a large area of interest in the fields of chemistry and pharmacy [1,2]
The HPMC polymer has a similar behavior as PAM-18, where the values obtained are close in magnitude and an increase in the hydrophobicity surface degree exist according to the polymer proportion
In the case of the hardness and disintegration time, these are most affected when the polymers used are ionic in nature, such as PAM-4Na and PAM-18Na, where greater interaction effects exist in the solid state, than when the polymers are neutral and hydrophobic, as PAM-18, where the hardness and disintegration times are very low
Summary
The development of new devices for controlled release of drugs corresponds to a large area of interest in the fields of chemistry and pharmacy [1,2] In this sense, different matrix systems of a polymeric character are used as a viable alternative with great potential for application in the design and formulation of pharmaceutical dosage forms [3,4,5]. Many polymeric materials have been used for this purpose, where the polymers derived from maleic anhydride are a worthwhile alternative, since they have shown great potential as controlled drug delivery systems [6,7,8,9,10,11,12] This class of polymers has attracted much attention due to the characteristics of biocompatibility, clearly defined structure and versatility to combine with other precursors to obtain materials with multiple properties and applications [13,14]. IItt iiss wwoorrtthhyy ttoo nnoottee tthhaatt aalltthhoouugghh mmaannyy ssttuuddiieess hhaavvee ddeessccrriibbeedd ddrruugg ddeelliivveerryy uussiinngg ppoollyymmeerriicc mmaatteerriiaallss,, tthheerree aarree vveerryy ffeeww ssttuuddiieess rreellaattiinngg tthhee rreelleeaassee mmeecchhaanniissmmss ffrroomm ccoommpprreesssseedd ttaabblleettss wwiitthh tthhee hhyyddrorpophhoboibciictiytydegdreegereoef thoef ptohlyemperoilcymmaetreicriamls aatnedriathlse saunrdfacethperospuerrftaiecseofptrhoeptearbtileests [o1f8–t2h0e]. tFaobrlethtsis[r1e8a–s2o0n]., tFhoisr wthoirskriesatshoenc, otnhtiisnwuaotrioknisofthaestcuodnytifnoucuatsieodnoonf eastsatbuldisyhifnogcuresleadtioonns ebsettawbeliesnhitnhge rseulraftaiocensthbeertmwoedenyntahme iscuprfraocpeetrhtieersmaonddyinnavmitircoprerolepaesretimeseachnadniinsmvsiturosirnegleaasmeomdeelchdarnuigsm(asmupsiicnilglina mtriohdyedlradtreu)gas(atmhepmiciolldinel tarnihdysdirmatiela)rapsotlhyememriocdmelaatenrdialssimwiiltahr dpioffleyrmenetridcemgraeteesrioaflshywdirthopdhioffbeirceintyt, dsuecghreaessPoAfMh-y4dNrao,pPhAobMic-i1t8yN, asuacnhd aPsAMPA-1M8.-4InNaad, dPiAtioMn-,1w8Ne ausaenddhyPdAroMx-y1l8-p. rIonpyald-dmietitohny,l-wceelluulsoesde (hHydPrMoxCy)l,-aprpooplyylm-mereitchmyl-acteelrliualloosef r(eHfePrMenCce), aandpowlyimdeelryicumseadteinriasltuodfieresfoerfemncoediafineddwreildeealsye u[2s1e–d23in]. sFtiundalileys, oitfsmhooudlidfiebde reexlpealasien[e2d1–th2a3t].wFeinuaslleyd, iatmshpoicuilldlinbetreihxypdlarianteedasthaamt woedeulsdedruagm(Fpiigcuilrlien1t)r,ihbeycdaruastee athseadmruogdheal sdaruragp(iFdigrautreeo1f)d, ibsseocaluutsioenthine tdhreupghhyassioalograicpaildmraedteiao, fthduisssaollluotwioinnginusthtoe rpelhaytesicohloagnigceasl minetdhiead, itshsuosluatilolonwpirnogfiluess atsosorceilaatteedcwhaitnhgaesmionditfiheeddrieslseoalsuetigoinvepnrboyfialens eaffsescotcoiafttehde pwoiltyhmaermicomdiaftireidx raenldeansoetgaivloenwbiyntarninesficfedctisosfoltuhteiopnoleyfmfecetri[c15m,2a4t]r.ix and not a low intrinsic dissolution effect [15,24]
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