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Purpose: The main aim of the present investigation was to enhance the solubility of poorly soluble Gliclazide by nanocrystallization.Methods: In present investigation gliclazide nanocrystals were prepared by sonoprecipitation using Pluronic F68, Poly Vinyl Alcohol (PVA), Poly ethylene Glycol 6000 (PEG), Poly Vinyl Pyrrolidine (PVP K30) and Sodium Lauryl Sulphate (SLS) as stabilizers. Fourier Transform Infrared Spectroscopic study (FTIR), Differential Scanning Calorimetry (DSC) and X ray diffraction (XRD) studies were conducted to study the drug interactions. Size and zeta potential of the nanocrystals were evaluated. In vitro and in vivo studies of nanocrystals were conducted in comparison to pure gliclazide.Results: The Gliclazide nanocrystals (GN) showed mean particle size of 131±7.7 nm with a zeta potential of -26.6 mV. Stable nanocrystals were formed with 0.5% of PEG 6000. FTIR, DSC and XRD studies of nanocrystals showed absence of interactions and polymorphism. SEM photographs showed a change in morphology of crystals from rod to irregular shape. There is an increase in the saturation solubility and the percentage drug release from formulation GN5 (Optimized Gliclazide Nanocrystals) was found to be 98.5 in 15 min. In the in vivo study, GN5 nanocrystals have reduced the blood glucose level to 296.4±4.26 mg/dl in 12 hr. The nanocrystals showed lower tmax and higher Cmax values as compared to pure gliclazide.Conclusion: The prepared nanocrystals of gliclazide were stable without any drug polymer interactions. Increase in the dissolution of nanocrystals compared to pure gliclazide and significant reduction in blood glucose level in vivo indicated better bioavailability of the nanocrystals. Therefore, it is concluded that nanocrystal technology can be a promising tool to improve solubility and hence dissolution of a hydrophobic drug.

The main objective of present study was to develop a buccal mucoadhesive drug delivery system for perindopril. Perindopril buccal mucoadhesive patches were developed by solvent casting technique using hydroxy propyl methylcellulose (HPMC), polycarbophil, sodium carboxymethylcellulose (SCMC) and sodium alginate as polymers for extended release of perindopril. Glycerine and DMSO were used as plasticizer and penetration enhancer respectively. Ethanol, methanol and dichloromethane were used as solvents. FTIR and DSC studies revealed no interaction between drug and polymers. The drug content in the perindopril patches was found to be uniform. The films exhibited good physical and mechanical properties. The surface pH of all the patches was within salivary pH range. Residual solvent content in patches are below the tolerated limits. The patches were found to have an extended release of the drug upto a period of 12 hours during ex vivo permeation studies with non-Fickian diffusion mechanism. The present study demonstrated the possibility of designing a buccal drug delivery system for perindopril.

Amaç: Bu çalışmanın amacı, kendiliğinden emülsifiye edici sistemlere formüle ederek, az çözünen ilaç indometazinin (IMN) çözünürlüğünü, çözünmesini ve dolayısıyla anti-inflamatuvar aktiviteyi arttırmaktır. Gereç ve Yöntemler: Kendi kendine emülsiyon haline getirici formülasyonlar yağ olarak capmul MCM, yüzey aktif madde olarak tween 80, kosürfaktant olarak transcutol P kullanılarak hazırlandı. İlaç ve eksipiyanlar arasındaki etkileşimi bilmek için fourier dönüşüm kızılötesi spektroskopisi ve diferansiyel tarama kalorimetrisi çalışmaları yapılmıştır. Pseudo üçlü faz diyagramları, kendinden emülsiyonlaşmış bölgeyi bilmek için 1:1 ile 1:4 ve 2:1 ile 4:1 arasında yüzey aktif madde ve kosürfaktant kullanılarak oluşturulmuştur. Formülasyonlar, parçacık büyüklüğü, zeta potansiyeli, kırılma indisi, viskozite ve bulut noktası açısından değerlendirildi. İn vitro çözünme çalışmaları, pH 7.2 fosfat tamponun bir bölümünde ve dört kısım suda gerçekleştirildi. Farmakokinetik parametreler Win Nonlin yazılımı ile analiz edildi. Bulgular: Kendiliğinden emülsifikasyon 2:1, 3:1 ve 1:2 oranında surfaktan ve kosürfaktant oranlarına göre daha yüksekti ve IMN formülasyonları hazırlandı. Formülasyonlar, farklı pH ve seyreltmelerde kararlıydı. Küre boyutu, 184.1 nm ile 340.5 nm aralığındaydı, çünkü yağ, yüzey aktif madde ve ko-yüzey aktif madde karışımı oranı kürenin boyutuna farklı etkiler yapmıştır. Tüm formülasyonların globüllerinin üzerindeki negatif yük, kararlılıklarına atıfta bulunmaktadır. Optimize edilmiş formülasyon, pazarlanan ürüne kıyasla daha iyi salınım gösterdi. Optimize edilmiş Kendi Kendine Emülsifiye Edici İlaç Taşıma Sistemi'nin AUC'si pazarlanan ürüne göre önemli derecede yüksekti. Sonuç: Böylece, mevcut araştırmadan kendi kendine emülsifiye IMN sistemleri, çözünmeyi ve dolayısıyla anti-inflamatuvar aktiviteyi arttırmak için yararlı bir alternatif sağlar. Anahtar kelimeler: Öz hazırlama için ilaç dağıtım sistemi, sözde üçlü faz diyagramı, zeta potansiyel, anti-inflamatuvar faaliyet, indometazin, AUC Objectives: The objective of the present study was to enhance the solubility, dissolution and hence anti-inflammatory activity of poorly soluble drug indomethacin (IMN) by formulating into self emulsifying systems. Materials and Methods: Self emulsifying formulations were prepared using capmul MCM as oil, tween 80 as surfactant, transcutol P as cosurfactant. Fourier transform infrared spectroscopy and differential scanning calorimetry studies were conducted to know the interaction between drug and excipients. Pseudo ternary phase diagrams were constructed using surfactant and cosurfactant in 1:1 to 1:4 and 2:1 to 4:1 to know the efficient self emulsification region. The formulations were evaluated for their particle size, zeta potential, refractive index, viscosity and cloud point. In vitro dissolution studies were conducted in one part of pH 7.2 phosphate buffer and four parts of water. The pharmacokinetic parameters were analysed by Win Nonlin software. Results: The self emulsification was higher with the ratios...

Objective: Glibenclamide is important and popular drug required in the treatment of hyperglycemia in Non-Insulin Dependent Diabetes Mellitus (NIDDM). Glibenclamide is affected by first pass metabolism and has a plasma half-life of 4 to 6 hrs, thus require high and frequent administration which in turn results in several side effect like nausea, vomiting, heartburn etc. To overcome this drawback glibenclamide was loaded into ethosomes to improve its therapeutic efficacy and decrease side effect via transdermal route.Six different ethosomal Material and methods: formulations with different concentration of ethanol, soya lecithin and cholesterol were prepared by cold method and characterized for vesicle size, polydispersity index (PI), zeta potential, vesicle surface morphology and entrapment efficiency (EE).permeation study was conducted using excised abdominal skin of rat as a permeation barrier Ex -vivo using franz diffusion cell.Formulation GF4 showed 7 fold higher (p<0.05) transdermal flux (56.08 ± 1.78 Results: µg/cm /hr) than the drug solution (7.64 ± 2.37 µg/cm /hr) and 3 fold higher than GF6 formulation (19.46 ± 2.64 2 2 µg/cm /hr). The high transdermal flux of GF4 formulation may be attributed to its smaller vesicle size (119.4 ± 1.1527 2 nm) and high entrapment efficiency. Based on the above findings the GF4 ethosomal formulation was converted to ethosomal gel formulation by incorporating it into 1% Carbopol 324 gel, which was further evaluated and compared with conventional gel formulation for skin permeability across the excised rat skin. Ethosomal gel Conclusion: formulation show significantly high (p<0.05) transdermal flux (37.23 ± 1.24 µg/cm /hr) as compared to conventional 2 gel formulation (16.35 ± 1.75 µg/cm /hr). It can be concluded that ethosomal gel formulations is an effective tool for 2 transdermal delivery of glibenclamide.