Development and evaluation of biodegradable microspheres embedded in in situ gel for controlled delivery of hydrophilic drug for treating oral infections: In vitro and in vivo studies
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Abstract
treat oral infections by using Poly (D, L lactic‑co‑glycolic) acid (50:50) as polymer. Microspheres were prepared using
oil‑in‑oil (O/O) and water‑in‑oil‑in‑water (W/O/W) double emulsion solvent evaporation method. Microspheres prepared
by W/O/W were spherical in shape compared those prepared with O/O method. Thus, the microspheres formulated by
W/O/W method were further evaluated for particle size, morphology, entrapment efficiency, and percent drug release.
Effects of salt addition, polymer concentration on the characteristics of microspheres and tetracycline release profile were
investigated. An increase in polymer concentration decreased drug release and increased entrapment efficiency of drug.
In vitro studies indicated that release of drug from microspheres could be controlled for 10-15 days depending on drug:
Polymer concentration. Formulation E released 99.10% of drug from microspheres in 10 days. Addition of sodium chloride
to outer aqueous phase produced spherical microspheres with smooth surface and also increased entrapment efficiency.
Microspheres were further dispersed in optimized formulation of mucoadhesive in situ gel of Pluronic F127, which acts
as carrier for microspheres. In vivo studies were conducted on patients who underwent molar tooth extraction to check
efficacy of designed formulation.
Key words: Double emulsion, in situ gel, microspheres, molar tooth extraction, poly (D, L lactic‑co‑glycolic) acid, tetracycline hydrochloride
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References
Xavier G. The importance of mouth care in preventing infection. Nurs
Stand 2000;14:47-51.
Sankar V, Hearnden V, Hull K, Juras DV, Greenberg MS, Kerr AR, et al. Local
drug delivery for oral mucosal diseases: Challenges and opportunities.
Oral Dis 2011;17 Suppl 1:73-84.
Schwach-Abdellaoui K, Vivien-Castioni N, Gurny R. Local delivery of
antimicrobial agents for the treatment of periodontal diseases. Eur J
Pharm Biopharm 2000;50:83-99.
Makadia HK, Siegel SJ. Poly lactic-co-glycolic acid (PLGA) as
biodegradable controlled drug delivery carrier. Polymers (Basel). 2011
;3:1377-1397.
Barman SP. Compositions and methods to prevent and treat dry
socket post-operatively after tooth extraction surgery. US Patent,
/0129801 A1.
Ng SM, Choi JY, Han HS, Huh JS, Lim JO. Novel microencapsulation
of potential drugs with low molecular weight and high
hydrophilicity: Hydrogen peroxide as a candidate compound. Int J
Pharm 2010;384:120-7.
Ito F, Fujimori H, Makino K. Incorporation of water-soluble drugs in
PLGA microspheres. Colloids Surf B Biointerfaces 2007;54:173-8.
Gaignaux A, Réeff J, Siepmann F, Siepmann J, De Vriese C, Goole J, et al.
Development and evaluation of sustained-release clonidine-loaded
PLGA microparticles. Int J Pharm 2012;437:20-8.
Kim HK, Chung HJ, Park TG. Biodegradable polymeric microspheres with
"open/closed" pores for sustained release of human growth hormone.
J Control Release 2006;112:167-74.
Mazumder B, Sarkar M, Dey S, Roy N. Effect of formulation and process
variables on the characteristics of microspheres of antiviral drug
(stavudine) prepared by oil-in-oil solvent evaporation technique. Int J
Pharm Pharm Sci 2012;2:52-9.
Meng FT, Ma GH, Qiu W, Su ZG. W/O/W double emulsion technique
using ethyl acetate as organic solvent: Effects of its diffusion rate on
the characteristics of microparticles. J Control Release 2003;91:407-16.
Reddy M, Firoz S, Rajalakshmi R, Ashok Kumar CK. Formulation and
In Vivo Evaluation of Oral Thermorevesible In Situ Gels Containing Anti
Fungal Drug. J pharm biol 2011;1: 20-4.
Kumar P, Awasthi R, Rai PK, Kumar M, Pramod Kumar TM. Mucoadhesive
in situ gels of local anaesthetic for periodontia. Der Pharmacia Lettre
; 2:28-39.
Daithankar AV, Shiradkar MR. Thermoreversibal anesthetic gel for
periodontal intrapocket delivery of mepivacaine hydrochloride. Der
Pharmacia Lettre 2012;4:889-96.
Patel B, Gupta V, Ahsan F. PEG-PLGA based large porous particles for
pulmonary delivery of a highly soluble drug, low molecular weight
heparin. J Control Release 2012;162:310-20.
Graves RA, Pamujula S, Moiseyev R, Freeman T, Bostanian LA, Mandal
TK. Effect of different ratios of high and low molecular weight PLGA
blend on the characteristics of pentamidine microcapsules. Int J Pharm
;270:251-62.
Yue IC, Poff J, Cortés ME, Sinisterra RD, Faris CB, Hildgen P, et al. A
novel polymeric chlorhexidine delivery device for the treatment of
periodontal disease. Biomaterials 2004;25:3743-50.
Block JB, Gary RJ. Prevention and treatment of alveolar osteitis. US
Patent, 2008/0241795 A1.
Carter DG. Techniques for prevention of alveolar osteitis. US Patent,
/5006071.