Comparison of Doxycycline Hyclate Release from Beta-Cyclodextrin Based In Situ Forming Systems for Periodontal Pocket Targeting

2020 ◽  
Vol 859 ◽  
pp. 120-124
Author(s):  
Sarun Tuntarawongsa ◽  
Jongjan Mahadlek ◽  
Nutdanai Lertsuphotvanit ◽  
Thawatchai Phaechamud

The release behavior of doxycycline hyclate (DH) from beta-cyclodextrin (β-CD) in situ gels (ISG) and in situ microparticles (ISM) was investigated using dialysis tube method and direct contact method compared to that from DH solution. From dialysis tube method, DH released completely from solution within 8 h, while it released with more sustainable from ISM and ISG completely at 12 h and 28 h, respectively. The release pattern of them was similar when tested using direct contact method (released completely at 9 days). The DH release from dialysis tube method of all systems was a first order kinetic. DH release from ISM using direct contact method fitted well with a Higuchi’s equation. The dialysis tube method was suitable for determining formula factors affecting the drug release behavior. However, to simulate the pocket condition with contact area is limited, the drug release test with direct contact method was preferred than dialysis tube method.

Author(s):  
Saruchi Sharma ◽  
VANEET KUMAR

Objective: This study involves the synthesis of Gum tragacanth (gt) based interpenetrating polymer network (ipn) and its utilization for sustained release of anti-ulcerative drug i.e. pantoprazole sodium. Methods: IPN was synthesized from Gum tragacanth, polyacrylic acid (gt-cl-paa) hydrogel. gt-cl-paa was kept in distilled water. Further, acryamide (aam) and methylmethacrylate (mma) was added and then kept for overnight. Later on, lipase and glutaraldehyde were added. Homopolymers and the unreacted monomers were removed using acetone. Synthesized IPN was dried at 50 °C for further study. Synthesized ipn was swelled in water and the drug was added to it. The drug was entrapped in the pores of the synthesized ipn and then drug release behavior was studied using uv-vis spectrophotometer. Results: Gt, paa and mma based crosslinked IPN were synthesized using lipase-glutaraldehyde as initiator-crosslinker system. The synthesized IPN was pH sensitive and possessed the desired swelling capacity required for the controlled and systematic liberation of pantoprazole sodium at 37 °C. The kinetic of drug release was studied and found that lateral diffusion (DL) of drug was higher as compared to the initial diffusion (DI). The prepared IPN can be used as prospective carrier for prolonged drug delivery. Conclusion: A novel pH sensitive and colon targeted IPN was synthesized. It acts as an effective device for the controlled release of drug pantoprazole sodium.


2013 ◽  
Vol 545 ◽  
pp. 63-68 ◽  
Author(s):  
Jongjan Mahadlek ◽  
Juree Charoenteeraboon ◽  
Thawatchai Phaechamud

Periodontitis is an inflammatory disease of the supporting structures of the tooth caused by bacterial infection which can result in tooth loss. The local intra-pocket drug delivery system was interesting and highly effective for periodontitis treatment. In situ forming gel system is the polymeric solution which could transform into gel for localizing and sustaining the drug release at desired site. This system has been recommended as one of suitable delivery system for this purpose. Benzoyl peroxide (BPO) in situ forming gels were developed using Eudragit RS as polymer dispersed in N-methyl-pyrrolidone (NMP). Peppermint oil and polyethylene glycol 1500 were also incorporated as the excipients. The prepared systems were evaluated for rheology, syringeability (using texture analyzers), in situ gel formation (after injection into PBS pH 6.8), antimicrobial activity (against Streptococcus mutans with agar diffusion) and drug release (with dialysis method in PBS pH 6.8 at 50 rpm, 37 °C). The viscosity and syringeability of the prepared systems was increased as the amount of BPO, peppermint oil or PEG 1500 was increased. All prepared gels showed the Newtonian flow which the viscosity was decreased as the temperature was increased. All prepared gels comprising peppermint oil and PEG 1500 could form in situ gel in used medium which the pH was close to the environment pH of periodontal pocket. The inhibition zone against Streptococcus mutans of the prepared system was significantly decreased when the peppermint oil and PEG 1500 was incorporated owing to the higher viscous environment and thereafter retardation of drug diffusion was evident. This effect could prolong the drug release. From drug release test, all prepared gels could sustain the BPO release for at least 96 hrs. Release kinetic obtained from curve fitting with various release equations using least square fit technique indicated that the release patterns were as Higuchi’s model therefore the release of BPO was performed with diffusion control. This developed BPO in situ forming gel presented its ability as the controlled drug delivery system for localized antimicrobial activity at periodontal pocket.


2008 ◽  
Vol 361 (1-2) ◽  
pp. 189-193 ◽  
Author(s):  
Qin Wang ◽  
Huibi Xu ◽  
Xiangliang Yang ◽  
Yajiang Yang

RSC Advances ◽  
2017 ◽  
Vol 7 (9) ◽  
pp. 5349-5361 ◽  
Author(s):  
LiNa Wang ◽  
Xiao Lin ◽  
YanLong Hong ◽  
Lan Shen ◽  
Yi Feng

To obtain a sustained in vivo release of Radix Ophiopogonis polysaccharide, hydrophobic solvent-induced in situ forming systems were investigated, including the factors affecting drug release and anti-myocardial ischemic activity of a formulation.


Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2275 ◽  
Author(s):  
Zhuanzhuan Yang ◽  
Xin Liang ◽  
Xiaojing Jiang ◽  
Jian Guo ◽  
Yaotian Tao ◽  
...  

In the present study, an injectable in situ liquid crystal formulation was developed for local delivery of minocycline hydrochloride (MH) for chronic periodontitis treatment. The physicochemical properties, phase structures, in vitro drug release and pharmacodynamics of in situ liquid crystals were investigated. The optimal formulation (phytantriol (PT)/propylene glycol (PG)/water, 63/27/10, w/w/w) loaded with 20 mg/g MH was proved to be injectable. The precursor formulation can form a cubic phase gel in excess water in 6.97 ± 0.10 s. The results of in vitro drug release suggested the MH presented a sustained release for 4 days. Liquid crystal precursor formulation significantly reduced gingival index, probing depth and alveolar bone loss compared to the model group (p < 0.01). Besides, the pathological characteristics of model rats were improved. The results suggested that MH-loaded in situ cubic liquid crystal possessed of sustained release ability and periodontal clinical symptoms improvement. The developed in situ cubic liquid crystal may be a potentially carrier in the local delivery of MH for periodontal diseases.


2020 ◽  
Vol 859 ◽  
pp. 21-26
Author(s):  
Setthapong Senarat ◽  
Juree Charoenteeraboon ◽  
Pitsiree Praphanwittaya ◽  
Thawatchai Phaechamud

With regard to the periodontal pocket application of in situ forming systems, the understanding the phase behavior after solidification owing to solvent movement could verify the deformability of specimen and its capacity to reside in the artificial periodontal pocket. The aim of this research was to investigate the phase behavior by determining mechanical properties as hardness and elasticity/plasticity ratio with texture analyzer for matrices obtained from drug-free and doxycycline hyclate (DX)-incorporated bleached shellac (BS) in situ forming gel (isg) and –microparticle (ism) after solvent exchange. The solvents for dissolving BS were 2-pyrrolidone (PYR), N-methyl pyrrolidone (NMP) and dimethyl sulfoxide (DMSO). The matrix from isg was less rough and bulge than that of isg. The order of mechanical hardness of transformed system prepared with different solvents was presented as PYR > NMP > DMSO, influenced by phase separation rate and porosity. The systems prepared with NMP and DMSO were more likely plastic or able to adapt its geometry to dynamic changes while that prepared with PYR was elastic. DX-incorporated ism matrix was still governed by the oil in external phase; thus, its consequence was reasonably plastic instead. XRD pattern indicated that the solvent type had no effect on the crystallinity of remained BS after solvent movement. SEM topography revealed sponge-like structure of isg prepared with DMSO and NMP whereas that prepared with PYR exhibited only initiated diminutive pores. The size and density of pores increased by time of isg using different solvents as following DMSO > NMP > PYR, whereas ism matrices had less pore density. The level of porosity of each matrix reflected the mechanical strength that a higher porous structure collapsed easily but a dense matrix considerably resisted to a compression.


2011 ◽  
Vol 19 (5) ◽  
pp. 515-518 ◽  
Author(s):  
Jong Rok Moon ◽  
Young Sil Jeon ◽  
Dong June Chung ◽  
Dukjoon Kim ◽  
Ji-Heung Kim

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