Preparation and evaluation of mucoadhesive bio-flexy films from Cocos nucifera biopolymer using Tiagabine moiety  

作　　者：Sugandha Varshney N.V.Satheesh Madhav 

机构地区：[1]Guru Nanak College of Pharmaceutical Sciences,Banshiwala,Jhajra,Dehradun,Uttarakhand,248007,India [2]Formulation Research Development,Vital Therapeutics and Formulations,Pvt.Ltd.,Telangana,500003,India

出　　处：《Precision Medicine Research》2021年第4期4-15,共12页精准医学研究

摘　　要：This research work deals with formulation and evaluation of nanosized Tiagabine loaded bio-flexy films consisting of Cocos nucifera biopolymer(isolated from coconut kernels).Prepared formulations were administered through soft palatal route for brain targeting for epilepsy treatment.Soft palate,part of oral mucosa serves as novel drug delivery platform and mucoadhesive site for systemic drug delivery.It provides sustained and controlled drug delivery system,does not interfere with patient’s regular activities like talking,eating,drinking,etc.It bypasses first-pass metabolism in the liver,reduces dose frequency and minimizes drug’s side effects.Tiagabine,anticonvulsant drug possesses t1/2:7-9 h(low);Protein binding:96%;Water solubility:22 mg/L,acts as selective gamma amino butyric acid(GABA)reuptake inhibitor.Cocos nucifera biopolymer used as bio-excipient to prepare bio-flexy films due to its biodegradability,biocompatibility,non-toxicity,non-irritantancy on soft palatal surface along with inbuilt filmability,mucoadhesive properties.Nanosized drug loaded bio-flexy films were formulated using standard solvent casting method.Bio-flexy films were prepared using varying ratios of nanosized Tiagabine:isolated Cocos nucifera biopolymer(FCT1-FCT6).These prepared formulations were compared with same ratios of nanosized Tiagabine:sodium carboxyl methyl cellulose standard polymer flexy films(FET1-FET6).The%yield of Cocos nucifera biopolymer was found to be 10.2±0.04%.Thickness of nanosized Tiagabine loaded bio-flexy films containing Cocos nucifera biopolymer(FCT1-FCT6)was ranging from 0.026±0.04 mm to 0.040±0.02 mm;Folding endurance:84-107;Surface pH:7.01±0.04 to 7.01±0.02;Weight uniformity:0.012±0.04 to 0.020±0.02;Drug content uniformity:69.5±0.35%to 72.9±0.26%;Swelling percentage:65±0.5%to 73±0.2%;Percentage moisture uptake(PTU):2.0±0.14%to 2.8±0.12%;Mucoadhesivity:20-90 min;Mucoretentivity:60-180 min.The drug release pattern for formulations FCT1-FCT6 containing Cocos nucifera biopolymer based on the T5

关 键 词：Nanosized Tiagabine Soft palatal delivery MUCOADHESIVE Cocos nucifera BIOPOLYMER Bio-flexy films 

分 类 号：R97[医药卫生—药品]