In e na ional Jou nal o Resea ch Publica ion and Re iews, Vol 6, Issue 10, pp 597-614, Oc obe , 2025
In e na ional Jou nal o Resea ch Publica ion and Re iews
Jou nal homepage: www.ij p .com ISSN 2582-7421
Fo mula ion and E alua ion o B i a ace am Loaded Nanosphe es
Ka hik V1*, Venka esh1, Salman M1, Hanuman hacha Joshi2.
1Depa men o Pha maceu ics, Sa ada Vilas College o Pha macy, Mysu u, Ka na aka, India
2Depa men o Pha macognosy, Sa ada Vilas College o Pha macy, Mysu u, Ka na aka, India
A B S T R A C T
The p esen s udy ocused on he de elopmen and e alua ion o B i a ace am-loaded nanosphe es using poly (lac ic-co-glycolic acid) (PLGA) as he polyme
ia he sol en e apo a ion me hod, aiming o enhance d ug solubili y, con ol elease, and imp o e he apeu ic e icacy. P e o mula ion s udies con i med ha
B i a ace am is a whi e o o -whi e, bi e - as ing, odou less d ug wi h high solubili y in wa e and a ious o ganic sol en s. The mel ing poin (131.97°C) and
FTIR, along wi h DSC analyses, con i med he d ug’s pu i y and compa ibili y wi h PLGA, showing no signi ican in e ac ions be ween d ug and polyme .
Nine nanosphe e o mula ions (F1–F9) we e de eloped and e alua ed. Pa icle size analysis e ealed ha o mula ion F5 had he smalles pa icle size (149.2 nm),
con ibu ing o i s imp o ed su ace a ea and s abili y. Ze a po en ial analysis showed F5 possessed he mos nega i e alue (–27.8 mV), indica ing excellen
colloidal s abili y. SEM imaging o F5 con i med uni o m sphe ical mo phology wi h minimal agg ega ion. D ug en apmen e iciency and d ug loading we e
highes in F5, a 79.4% and 12.3%, espec i ely, signi ying e ec i e d ug encapsula ion and op imal polyme in e ac ion.
In i o dissolu ion s udies demons a ed sus ained d ug elease ac oss all o mula ions o e 12 hou s, wi h F5 showing he highes cumula i e elease o 85.3%
o nanosphe es and 95.6% o capsule o mula ions, con i ming i s supe io elease p o ile. Capsule e alua ion pa ame e s including weigh a ia ion,
disin eg a ion ime, and d ug con en uni o mi y emained wi hin pha macopeial limi s, wi h F5 again displaying he mos a ou able esul s (disin eg a ion ime:
18 min; d ug con en : 98.7%).
O e all, he da a alida e he success o he sol en e apo a ion me hod o o mula ing B i a ace am nanosphe es using PLGA, and among all he de eloped
o mula ions, F5 eme ged as he mos op imized o mula ion.
Keywo ds: B i a ace am, PLGA, Nanosphe es, Encapsula ion
1. INTRODUCTION
The Nano D ug Deli e y Sys em (NDDS) is a dynamic a ea o scien i ic esea ch, d i en by he apid ad ancemen s in nano echnology. This ield
ocuses on he inno a i e de elopmen o d ug deli e y me hods ha le e age nanoscale ma e ials o enhance he apeu ic e icacy and p ecision.[1] I
in ol es he in es iga ion o indi idual molecules, a oms, o compounds o c ea e s uc u es ha exhibi unique p ope ies.[2] Nano echnology wi h a
wide ange o nanoca ie s such as liposomes and nanopa icles ocused on a ge ed d ug deli e y has been expanding quickly. [3] Nanopa icles (NPs)
a e one o he nano sys em deli e y me hods which ha e been de eloped o accomplish ex ended o o ganized d ug deli e y, o inc ease he
bioa ailabili y, d ug s abili y, and d ug a ge ing o he si e o ac ion. Nanosphe es a e small pa icles wi h a size ange o 10 o 200 nm.[4]
Epilepsy is conside ed one o he mos p e alen neu ological illnesses, a ec s mo e han 50 million people wo ldwide, and each yea app oxima ely 5
million new cases a e diagnosed. Epilepsy is cha ac e ized by abe an b ain ac i i y esul ing in con ulsions. Depending on basic b ain dys unc ions,
his neu ological diso de comp ises nume ous e iologies including ab up and excessi e neu onal discha ges ha esul in epilep ogenesis. Al hough i
a ec s people o all ages, he a e o disease is high in child en and elde ly pe sons.[5]
Nano D ug Deli e y Sys ems (NDDS) can p olong he p esence o d ugs in he bloods eam, esul ing in educed luc ua ions in plasma le els and
consequen ly minimizing side e ec s. These nanosphe es enable a ge ed d ug deli e y, which is c ucial o e ec i ely managing epilepsy.[6][7]
1.1 Ad an ages o Nanosphe es
E icien Pene a ion: Nanosphe es can eadily a e se e en he smalles capilla y essels, ensu ing e ec i e dis ibu ion h oughou he
body.
Ta ge ed O gan Deli e y: They can be u ilized o speci ically a ge o gans such as he li e , spleen, lungs, and spinal co d, enhancing
he apeu ic p ecision.[8]
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Dec eased Toxici y: Nanosphe es help lowe oxici y le els and educe he equency o equi ed dosages.
Ve sa ile Adminis a ion Me hods: They can be adminis e ed h ough mul iple ou es, including o al, nasal, and pa en e al op ions.
Quick Clea ance and Ta ge ed Deli e y: Nanosphe es enable apid clea ance om he bloods eam while allowing o p ecise a ge ing a
speci ic si es wi hin he body.[9]
1.2 Disad an ages o Nanosphe es
Handling Challenges: Nanosphe es can be di icul o manage in bo h liquid and d y o ms.
Manu ac u ing Expe ise Requi ed: The p oduc ion o nanosphe es demands specialized skills and echniques.
Suscep ibili y o Agg ega ion: Due o hei small size and la ge su ace a ea, nanosphe es a e p one o pa icle agg ega ion.[10]
1.3 EPILEPSY
Epilepsy is a neu ological diso de which is cha ac e ized by epea ed seizu es and known o a ec s people o all age g oup. Seizu es a e elec ical
impulses discha ged by ne e cells p esen in he b ain. Possible easons o seizu es a e head inju ies, abno mal b ain de elopmen , gene ic and
in ec ious illness (meningi is). The d ugs used o he ea men o epilep ic seizu es a e known as an iepilep ic d ugs which a e known o dec ease he
equency o se e i y o seizu es.
Mos o he an iepilep ic d ug’s ac by any o hese h ee mechanisms;
Modula ion o ol age ga ed ion channels,
Enhancemen o gamma amino bu y ic acid (GABA) media ed inhibi o y neu o ansmission
By glu ama e media ed exci a o y neu o ansmission.
1.4 Capsules
Capsules a e uni solid dosage o ms ha se e as small con aine s (shells) made p ima ily o gela ine, enclosing accu a ely measu ed amoun s o d ug
subs ances. The e m “capsule” comes om he La in wo d capsula, meaning “small con aine .” Capsules hold a signi ican ole in d ug de elopmen
and a e o en conside ed a p ima y o al dosage o m due o he simplici y o hei manu ac u ing p ocess compa ed o o he dosage o ms. Besides
gela ine, ma e ials such as dena u ed gela ine, me hylcellulose, and poly inyl alcohol can be used o capsule shells.
Capsules a e mainly o wo ypes: ha d-shelled capsules, con aining d y powde s o pelle s p oduced h ough p ocesses like ex usion o sphe oniza ion,
and so -shelled capsules, con aining liquids o semi-solids. Ha d capsules consis o wo pa s a smalle “body” and a la ge “cap” which i oge he .
Bo h ypes a e made om aqueous solu ions o gelling agen s (animal p o eins like gela ine o plan polysaccha ides), wi h added plas icize s (e.g.,
glyce ine, so bi ol) o adjus shell ha dness.[11,12]
Ad an ages o Capsules
Fewe de elopmen al issues, enabling quicke submission o new d ugs o clinical ials.
Easie o a y he dose compa ed o o he dosage o ms.
Requi e ewe excipien s han able s.
Manu ac u ing in ol es ewe s eps han able p oduc ion.
Easy o swallow, enhancing pa ien compliance.
Allow simple sepa a ion o wo incompa ible d ugs wi hin he same dosage uni .
O e g ea e possibili ies o p oduc iden i ica ion h ough p in ing.
Sui able o inco po a ing d ugs wi h high doses and low comp essibili y. [13]
Disad an ages o Capsules
Capsules a e unsui able o liquids ha can dissol e gela in, such as aqueous o hyd oalcoholic solu ions.
Concen a ed solu ions equi ing p io dilu ion a e no sui able o encapsula ion, as di ec adminis a ion may cause gas ic
i i a ion.
Types o capsules
I. Ha d gela ine capsule.
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II. So gela ine capsule.
Fig 4: ypes o capsules
1.5 Filling o ha d gela ine capsules
The p ocess o illing ha d gela ine capsules is a well-es ablished echnology, wi h equipmen op ions anging om small-scale manual de ices (e.g.,
Fe on capsule illing machine) o medium-scale semi-au oma ic machines and la ge-scale ully au oma ic sys ems. In compounding pha macies,
capsules may also be illed manually, one a a ime.
2. MATERIALS AND METHODS
2.1 PRE-FORMULATION STUDIES:
P e- o mula ion may be desc ibed as he s age o de elopmen du ing which he physicochemical and biopha maceu ical p ope ies o a d ug subs ance
a e cha ac e ized. I is an impo an pa o he d ug de elopmen p ocess. The in o ma ion ela ing o d ug de elopmen acqui ed du ing his phase is
used o making c i ical decisions in subsequen s ages o de elopmen . A wide a ie y o in o ma ion mus be gene a ed o de elop o mula ions
a ionally. Cha ac e iza ion o he d ug is a e y impo an s ep a he p e- o mula ion phase o p oduc de elopmen ollowed by s udying he
p ope ies o he excipien s on hei compa ibili y.
2.1.1 O ganolep ic p ope ies o B i a ace am:
Small sample o B i a ace am was aken in Pe i dish, sp ead ca e ully and de e mine he colou , odou and ex u e. and he obse a ions a e shown in
able 4.
2.1.2 Solubili y:
Solubili y is exp essed in e ms o pa s pe million o sol en in which 1g o solid is soluble. Solubili y o he powde in a ious sol en s a 20°C. [14]
2.1.3 Mel ing poin :
The mel ing poin was ca ied ou by using capilla y ube me hod. A small sample o B i a ace am was placed in a glass capilla y ube ha had been
p e iously sealed on one end. The d ug- illed capilla y ube was hen placed inside he mel ing poin appa a us, and he empe a u e a which he d ug
began o mel was moni o ed using a he mome e .[15]
SL.NO
Ing edien s
Manu ac u e
1
B i a ace am
Mic o labs, Bangalo e.
2
PLGA (poly lac ic co glycolic acid)
Venus Lab P oduc s, Bangalo e.
3
PVA (Poly Vinyl Alcohol)
Ka na aka Fine Chem, Bangalo e.
4
(DCM)Dichlo ome hane
Sisco Resea ch Labo a o ies P . L d, New
Mumbai.
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2.2 Compa ibili y S udies
2.2.1 FTIR Spec oscopy
FTIR s udy was ca ied ou o check he compa ibili y o d ug wi h polyme s. In a ed spec um o B i a ace am was de e mined on Fou ie ans o m
In a ed spec opho ome e using KB dispe sion me hod. The baseline co ela ion was done using d ied po assium b omide. Then he spec um o
d ied mix u e o d ug and Po assium b omide was un ollowed by d ug wi h a ious polyme s by using FTIR spec opho ome e . The abso p ion
maximums in spec um ob ained wi h he subs ance being examined co espond in posi ion and ela i e in ensi y o hose in he e e ence spec um. [16]
and he obse a ions a e shown in Figu e11 and 12.
2.2.2 Di e en ial Scanning Calo ime y s udies o B i a ace am
To in es iga e he physical and chemical in e ac ions be ween he medicine and he applied excipien s, Di e en ial Scanning Calo ime y (DSC) was
used. On he DSC-60 equipmen , DSC spec a o pu e d ugs and d ug composi e mix u es we e cap u ed. The d ug-excipien mix u e was scanned in a
ni ogen- illed en i onmen be ween 50 and 400°C. All samples we e p epa ed in aluminium pans wi h aluminium co e s. The he mog ams we e
obse ed o any kind o in e ac ion a a hea ing a e o 20 °C/min. [17] and he obse a ions a e shown in Figu e 13 and 14.
2.3 Analy ical me hod used in de e mina ion o B i a ace am
S anda d Cu e o B i a ace am
S ock solu ion was p epa ed by using 50 mg o B i a ace am in 100 ml o phospha e bu e (pH 6.8). F om his s ock solu ion 10 ml was wi hd awn
and dilu ed up o 100 ml using wa e . Calib a ion cu e was p epa ed by using di e en concen a ion (5µg/ml-30 µg/ml) by app op ia e dilu ion o
s ock solu ion. The abso bance was measu ed a 272 nm. [18] and he obse a ions a e shown in Figu e 15.
2.4 FORMULATION DEVELOPMENT OF BRIVARACETAM BY SOLVENT EVAPORATION METHOD
Table-3: Fo mula ion ials o nanosphe e wi h B i a ace am
Ing edien s
F1
F2
F3
F4
F5
F6
F7
F8
F9
B i a ace am in (g)
0.1
0.1
0.1
0.1
0.1
0.1
0.1
0.1
0.1
Poly lac ic co glycolic acid (PLGA) (g)
5.0
6.0
7.0
5.0
6.0
7.0
5.0
6.0
7.0
Poly Vinyl Alcohol (PVA) (g)
0.1
0.1
0.1
0.2
0.2
0.2
0.25
0.25
0.25
Dichlo ome hane (DCM) (ml)
5
5
5
5
5
5
5
5
5
Dis illed wa e (ml)
25
25
25
25
25
25
25
25
25
To al (g)
35.2
36.2
37.2
35.3
36.3
37.3
35.35
36.35
37.35
P ocedu e:
2.4.1 P epa a ion o O ganic Phase:
Dissol e B i a ace am (100 mg) and PLGA (600 mg) in 5mL o DCM.
Mix ho oughly un il a clea o ganic solu ion is o med.
2.4.2P epa a ion o Aqueous Phase:
P epa e 1% PVA solu ion by dissol ing 1 g o PVA in 100 mL dis illed wa e while con inuously hea ing and s i ing.
2.4.3 Emulsi ica ion:
Slowly add he o ganic phase d opwise in o he aqueous phase (unde magne ic s i ing a 1000–1500 pm).
Con inue s i ing o 2–3 hou s a oom empe a u e o allow DCM o e apo a e.
2.4.4 Collec ion o Nanosphe es:
Cen i uge he esul ing emulsion a 15,000 pm o 30 minu es.
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Disca d he supe na an and wash he nanosphe es wi h dis illed wa e 2–3 imes.
2.5 Capsule Filling P ocedu e
The op imized nano sphe ic o mula ion was d ied comple ely and weighed accu a ely. The amoun equi alen o he equi ed dose o B i a ace am
was illed in o size ‘0’ ha d gela ine capsules manually using a capsule illing machine. Ca e was aken o ensu e uni o mi y in capsule weigh and
con en . Each capsule was s o ed in a desicca o un il e alua ion.[19]
Figu e 10: Fo mula ion o B i a ace am loaded nanosphe e.
2.6 EVALUATION OF NANOSPHERE
2.6.1 Pa icle Size Dis ibu ion
The pa icle size and dis ibu ion a e one o he mos impo an cha ac e is ics o nanopa icle sys ems. Immedia ely a e p ecipi a ion, he size o he
d ug nanosphe es was measu ed using dynamic lase ligh sca e ing wi h a nanopa icle size analyze (Mal e n). The d ug solu ion was dilu ed o a
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concen a ion o 0.2 mg/mL wi h pu i ied wa e p io o analysis. The esul s om he pa icle size s udy we e in e p e ed using he g aphic mean size
(Mz) and calcula ed su ace a ea. [20][21] and he obse a ions a e shown in Table 08 and Figu e 16.
2.6.2 Ze a Po en ial
The size, size dis ibu ion, and ze a po en ial o he nanosphe es we e assessed using a ze a size (ZS 90 Mal e n). P io o es ing, he lyophilized
samples we e dilu ed wi h PBS o achie e a concen a ion o 1 mg/mL and a pH o 6.0. These samples we e placed in a clean cu e e du ing he size
analysis o ob ain mul iple peaks, which we e hen used o calcula e he a e age ze a size. Fo he ze a po en ial measu emen s, he samples we e kep
in he analysis chambe o he ze a size while i was ope a ional o collec accu a e da a. Typically, he ocus is on he monodispe se cha ac e is ics o
his da a a he han i s polydispe se aspec s.[22][23] and he obse a ions a e shown in Table 09 and Figu e 17,18 &19.
2.6.3 D ug En apmen E iciency (EE%) and D ug Loading (DL%)
To de e mine he d ug en apmen e iciency (EE%) and d ug loading (DL%), he nanosphe es unde go a p ocess o cen i uga ion, washing, e-
cen i uga ion, and subsequen il a ion. An aliquo o he supe na an is aken and dilu ed o analysis. The concen a ion o he ee d ug is measu ed
using a UV-Visible spec opho ome e . The amoun o en apped d ug is calcula ed by sub ac ing he quan i y o ee d ug om he o al amoun o
d ug ini ially added o he o mula ion. [24] and he obse a ions a e shown in Table 10 & 11 and Figu e 22 & 23.
Calcula ing he o mula:
EE (W/W) % = Amoun o en apped d ug × 100
To al amoun o he d ug added
DL (W/W) % = Amoun o en apped d ug × 100
(amoun o polyme + en apped d ug)
2.6.4 Scanning Elec on Mic oscopy (SEM)
The pa icle mo phology o bo h un ea ed and ea ed d ug nanosphe es was analysed using scanning elec on mic oscopy. Each d ug powde sample
was di ided in o small pieces and a ixed o double-sided ca bon conduc i e ape. A P -Pd alloy coa ing, app oxima ely 5 nm hick, was hen applied o
co e he en i e su ace o he ape. Mic og aphs we e cap u ed using a Zeiss DSM 982 Field Emission Gun Scanning Elec on Mic oscope (Ca l Zeiss
AG, Ge many). [25] and he obse a ions a e shown in Figu e 20 & 21.
2.6.5 Modi ied Dissolu ion Tes
The in i o d ug elease s udy by he memb ane di usion me hod in ol es soaking a dialysis memb ane in dis illed wa e o e nigh , hen insing wi h
phospha e bu e . A ixed olume o he nanosphe e o mula ion is placed inside he memb ane, which is sealed and imme sed in 100 mL o phospha e
bu e (pH 6.8 o 7.4) a 37 ± 0.5 °C wi h con inuous s i ing. A speci ic ime in e als, 1 mL o he sample is wi hd awn and eplaced wi h esh bu e .
D ug elease is analyzed using a UV spec opho ome e , and cumula i e pe cen age elease is calcula ed and plo ed agains ime o s udy he elease
kine ics and p o ile. [26] and he obse a ions a e shown in Table 12 and Figu e 24,25 & 26.
2.7 EVALUATION OF BRIVARACETAM LOADED NANOSPHERE CAPSULES
Weigh Va ia ion
Disin eg a ion Time
D ug Con en Uni o mi y
In i o D ug Release
2.7.1 Weigh Va ia ion:
20 capsules a e selec ed o aken a andomly and weighed indi idually, ake a e age and compa e each capsule weigh wi h a e age. Then es
passes i none o he indi idual weigh s a e less han 90% and mo e han 110% o a e age. I es equi emen s a e no me , we ha e o emo e he
powde , ne con en o powde can be weighed indi idually. They ha e o be a e aged. Tes equi emen s a e me i no mo e han 2 o he
indi idual's di e ence is no g ea e han10 o a e age. In any case di e ence should no be mo e han o equal o 25%. I mo e han 2 and less han 6
ne weigh s de e mined, hey de ia e 10% Then we go o addi ional 40 capsules. The a e age o 60 capsules is de e mined by weighing capsules
indi idually and compa ed wi h a e age.[27] and he obse a ions a e shown in Table 13.
Pe cen age De ia ion (%) =�����������������������−�������������
������������ ���
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2.7.2 Disin eg a ion Time:
The capsules a e placed in he baske - ack assembly, which is epea edly lowe ed 30 imes pe minu e in o a he mos a ically con olled ba h o luid
a 37 +2°C and obse ed o e he ime desc ibed in he indi idual monog aph. [27] and he obse a ions a e shown in Table 14 and Figu e 27.
2.7.3 D ug Con en Uni o mi y:
This es is equi ed only when speci ied in indi idual monog aphs o when capsules ail he weigh a ia ion es . I he capsules a e comple ely
illed, he es is no necessa y. Unless o he wise s a ed in he monog aph o a speci ic capsule, he d ug con en de e mined by assay should all
wi hin 85.0% o 115.0% o he labelled claim in a leas nine ou o en dosage uni s, wi h no single uni ou side 75.0% o 125% o he labelled
con en . Addi ional es ing is equi ed i wo o h ee dosage uni s all ou side he accep able ange bu emain wi hin he s a ed limi s.[27] and he
obse a ions a e shown in Table 15.
2.7. 4 In i o D ug Release:
The elease p o ile was s udied using he IP Dissolu ion Tes Appa a us Type II (baske ype). The baske was imme sed in 900 ml o phospha e
bu e (pH 6.8) main ained a 37 ± 0.5°C, wi h he appa a us ope a ed a 50 pm. A i e-minu e in e als o up o 60 minu es, 5 ml o he medium
was wi hd awn, il e ed h ough Wha man No. 41 il e pape , and eplaced wi h esh bu e . Abso bance was eco ded a 272 nm, and cumula i e
d ug elease was calcula ed om he calib a ion cu e.[27] and he obse a ions a e shown in Table 16 Figu e 28,29& 30.
3. RESULTS AND DISCUSSION
3.1 PREFORMULATION STUDIES
3.1.1 O ganolep ic p ope y o B i a ace am
The o ganolep ic p ope ies like colou , odou , and as e o he excipien s we e e alua ed and he obse a ion shown in able 4.
Table 4: O ganolep ic p ope y o B i a ace am
3.1.2 Solubili y
Solubili y is exp essed in e ms o pa s pe million o sol en in which 1g o solid is soluble. Solubili y o he powde in di e en sol en s like e hanol
was de e mined a 20°C. The solubili y s udies o d ug e ealed ha , B i a ace am is highly soluble in a ious sol en s. I is eely soluble in wa e ,
bu e (pH 1.2, 4.5, 7.4), E hanol, Dichlo ome hane, Me hanol and Glacial ace ic acid, Soluble in Ace one, Toluene and sligh ly soluble in n- hexane.
B i a ace am has a solubili y o 21.23 mg/ml in bo h DMSO and wa e . Hence B i a ace am exhibi s excellen solubili y in wa e and common o ganic
sol en s, which acili a es i s o mula ion and adminis a ion.
3.1.3 Mel ing poin de e mina ion
The mel ing poin was ca ied ou by using capilla y ube me hod. The esul ound o be 131.97°C. Hence complies wi h USP s anda d, hus indica es
he pu i y o he d ug sample.
3.1.4 FTIR s udies o B i a ace am
The ac i e componen B i a ace am and physical mix u e wi h di e en polyme s we e aken o FTIR. The FTIR spec um o B i a ace am and
mix u e o B i a ace am wi h polyme was gi en in he ig 11 and 12
Tes
Obse a ion
Colou
Whi e o o whi e
Odou
Odou less
Tas e
Bi e
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Figu e 11: FTIR Spec a o B i a ace am Figu e 12: FTIR Spec a o B i a ace am and PLGA
Table 5: Compa ison peak o unc ional g oups o B i a ace am obse ed in FTIR spec a o compa ibili y s udies
The FTIR compa ibili y s udy be ween B i a ace am and PLGA was e alua ed by compa ing he cha ac e is ic peaks o he d ug, physical mix u e, and
o mula ion. The O–H s e ching ib a ion appea ed a 3292.60 cm⁻¹ o B i a ace am, 3315.74 cm⁻¹ in he physical mix u e, and 3310.10 cm⁻¹ in he
o mula ion, indica ing sligh shi s. N–H s e ching was obse ed a 2914.54 cm⁻¹ in he d ug, 2831.76 cm⁻¹ in he mix u e, and 2842.45 cm⁻¹ in he
o mula ion. C–H s e ching showed peaks a 2848.96 cm⁻¹ o B i a ace am, 2819.68 cm⁻¹ in he mix u e, and 2814.76 cm⁻¹ in he o mula ion. The
C–N s e ching ib a ion was no ed a 2237.50 cm⁻¹ o he d ug, 2249.61 cm⁻¹ in he mix u e, and 2247.81 cm⁻¹ in he o mula ion. The C=O
s e ching ib a ion, a key unc ional g oup in amide bonds, appea ed a 1656.91 cm⁻¹ in he d ug, 1659.79 cm⁻¹ in he mix u e, and 1654.31 cm⁻¹ in he
o mula ion. Las ly, C–C s e ching appea ed a ound 1406–1401 cm⁻¹ ac oss all samples. The e en ion o all majo peaks wi h mino shi s indica es no
signi ican chemical in e ac ion, con i ming good compa ibili y be ween B i a ace am and PLGA.
3.1.5 Di e en ial Scanning Calo ime y s udies o B i a ace am
Physical incompa ibili y s udy was ca ied ou by DSC. Due o i s alue in s udying solid-s a e in e ac ions, he mog ams we e p oduced o mix u es
con aining bo h pu e d ugs and d ug excipien s.
The e was no in e ac ion be ween he medica ion and he polyme s, acco ding o he DSC s udy. The e was no disce nible a ia ion in he mel ing
endo he ms o he d ugs physical combina ion con aining all polyme s, and he he mog ams o DSC e ealed he endo he mic peak o he pu e d ug a
102°C.
The esul s showed ha he selec ed d ug and he polyme s we e physically compa ible. The DSC esul s we e ep esen ed in Table 6 and DSC
he mog ams a e shown in ig.13 And 14.
Sl. No
Types o Vib a ion
B i a ace am (cm-1)
Physical Mix u e
(D ug+ PLGA) (cm-1)
1
O-H S e ching
3292.60
3315.74
2
N-H S e ching
2914.54
2831.76
3
C-H S e ching
2848.96
2819.68
4
C-N S e ching
2237.50
2249.61
5
C=O s e ching
1656.91
1659.79
6
C-C s e ching
1406.15
1401.25
In e na ional Jou nal o Resea ch Publica ion and Re iews, Vol 6, Issue 10, pp 597-614 Oc obe , 2025 605
Figu e 13: DSC o B i a ace am Figu e 14: DSC o B i a ace am and PLGA
The DSC he mog am o pu e B i a ace am shows a sha p endo he mic peak a app oxima ely 102°C, co esponding o i s mel ing poin and
con i ming i s c ys alline na u e and pu i y. PLGA exhibi s a glass ansi ion empe a u e (Tg) a ound 47.4°C, wi h a mino ansi ion nea 52.0°C,
indica ing i s amo phous cha ac e and polyme mobili y. In he physical mix u e o B i a ace am and PLGA, he mel ing peak o he d ug is
signi ican ly educed o absen , his shi indica es success ul molecula dispe sion o B i a ace am wi hin he PLGA ma ix, suppo ing he o ma ion
o a solid dispe sion o encapsula ed sys em.
Table 6: DSC esul s om he he mog ams o bo h d ug and physical mix u e o d ug- excipien s
Sl.no
Sample
Endo he mic peak
1
B i a ace am
102 °C
2
B i a ace am + PLGA
52 °C
DSC analysis showed ha B i a ace am has a sha p mel ing peak a ~101°C, con i ming i s c ys alline na u e, while PLGA displayed a glass ansi ion
a ound 52°C. In he physical mix u e, he d ug's peak was sligh ly shi ed and educed, indica ing no majo in e ac ion bu good compa ibili y. These
esul s con i m he he mal s abili y o B i a ace am wi h PLGA.
3.1.6 S anda d G aph o B i a ace am
S ock solu ion was p epa ed by using 50 mg o B i a ace am in 100 ml o phospha e bu e (pH 6.8). F om his s ock solu ion 10 ml was wi hd awn
and dilu ed up o 100 ml using wa e . Calib a ion cu e was p epa ed by using di e en concen a ion (5µg/ml-30 µg/ml) by app op ia e dilu ion o
s ock solu ion. The abso bance was measu ed a 272 nm.
Table 7: S anda d G aph o B i a ace am
Sl no
Concen a ion µg/ml
Abso bance
1
0
0
2
5
0.159 ± 0.03
3
10
0.326 ± 0.01
4
15
0.525 ± 0.05
5
20
0.661 ± 0.02
6
25
0.821 ± 0.01
7
30
0.941 ± 0.04
In e na ional Jou nal o Resea ch Publica ion and Re iews, Vol 6, Issue 10, pp 597-614 Oc obe , 2025 612
Fo mula ions
Disin eg a ion Time
(Min)
Pha macopeial Limi (<30
Min)
Resul
F4
19
<30 Min
Complies
F5
18
<30 Min
Complies
F6
21
<30 Min
Complies
F7
26
<30 Min
Complies
F8
23
<30 Min
Complies
F9
25
<30 Min
Complies
Figu e 28: Disin eg a ion Time (Min) o he Fo mula ions F1-F9
3.3.3 D ug Con en Uni o mi y (%):
The d ug con en uni o mi y o B i a ace am nanosphe e-loaded capsules was ound o be consis en ac oss all o mula ions, wi h alues anging om
94.2% o 98.7%. Fo mula ion F1 exhibi ed a uni o mi y o 96.2 ± 1.3%, while F2 showed a sligh ly highe alue o 97.1 ± 1.1%. F3 eco ded 95.3 ±
1.4%, whe eas F4 and F5 demons a ed compa a i ely highe uni o mi y a 98.0 ± 1.2% and 98.7 ± 1.0%, espec i ely. F6 also main ained a
sa is ac o y le el wi h 97.5 ± 1.3%. On he o he hand, o mula ions F7, F8, and F9 showed ela i ely lowe alues o 94.8 ± 1.5%, 95.7 ± 1.3%, and
94.2 ± 1.6%, espec i ely. O e all, all o mula ions we e wi hin he accep able pha macopeial limi s, ensu ing good con en uni o mi y
.Table 15: D ug Con en Uni o mi y
Fo mula ions
D ug Con en Uni o mi y
(%)
Pha macopeial Limi (85–
115%)
Resul
F1
96.2 ± 1.3
85–115%
Complies
F2
97.1 ± 1.1
85–115%
Complies
F3
95.3 ± 1.4
85–115%
Complies
F4
98.0 ± 1.2
85–115%
Complies
F5
98.7 ± 1.0
85–115%
Complies
F6
97.5 ± 1.3
85–115%
Complies
F7
94.8 ± 1.5
85–115%
Complies
F8
95.7 ± 1.3
85–115%
Complies
F9
94.2 ± 1.6
85–115%
Complies
In e na ional Jou nal o Resea ch Publica ion and Re iews, Vol 6, Issue 10, pp 597-614 Oc obe , 2025 613
3.3.4 In- i o Dissolu ion S udy o B i a ace am Nanosphe e Capsules
The in- i o d ug elease s udy o B i a ace am-loaded nanosphe e capsules was pe o med using he USP Type II (paddle) appa a us in 900 mL o
phospha e bu e (pH 6.8) a 50 pm and 37 ± 0.5 °C. Samples we e wi hd awn a p ede e mined in e als (0.5–12 h), il e ed, and analyzed
spec opho ome ically. The esul s a e shown below.
Table 16: In- i o Dissolu ion S udy o B i a ace am Nanosphe e Capsules
Time(h)
F1
F2
F3
F4
F5
F6
F7
F8
F9
0.5
18.5
20.4
17.8
21.1
22.6
20.8
15.6
16.2
14.9
1.0
28.7
30.2
27.5
31.6
33.4
30.8
25.2
26.0
23.8
2.0
41.3
44.6
39.8
46.2
48.7
45.1
36.6
37.8
34.4
3.0
52.5
55.9
50.8
58.4
61.1
57.2
46.2
47.5
43.9
4.0
63.1
66.5
61.7
69.3
72.4
68.2
55.6
56.8
52.7
6.0
74.6
77.8
72.2
80.1
83.6
79.2
65.8
67.4
63.9
8.0
81.2
84.7
79.6
86.4
89.2
85.5
76.8
78.4
74.9
10.0
84.8
87.9
82.6
89.3
92.1
88.6
79.9
81.3
77.8
12.0
88.6
91.3
86.5
92.7
95.6
92.2
83.5
85.1
81.2
Figu e 29: Cumula i e % D ug Release (F1–F3), (F4-F6), (F7-F9) showing he compa a i e d ug elease p o iles.
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