scholarly journals Novel application of mixed solvency concept in the development of oral liquisolid system of a poorly soluble drug, cefixime and its evaluation

2018 ◽  
Vol 8 (6-s) ◽  
pp. 5-8 ◽  
Author(s):  
Rinshi Agrawal ◽  
RK Maheshwari
Keyword(s):  
Drug Loading ◽  
Research Work ◽  
Water Soluble ◽  
Dsc Studies ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Soluble Drug ◽  
Model Drug ◽  
Poorly Water Soluble Drug

Application of mixed solvency has been employed in the present research work to develop a liquisolid system (Powder formulation) of poorly water soluble drug, cefixime (as model drug). Material and Methods: For poorly water soluble drug cefixime, combination of solubilizers such as sodium acetate, sodium caprylate and propylene glycol as mixed solvent systems were used to decrease the overall concentration of solubilizers required to produce substantial increase in solubility and thereby resulting in enhanced drug loading capacity of cefixime. The procured sample of cefixime was characterized by melting point, IR, UV and DSC studies. Stability studies of liquisolid system of cefixime were performed for two months at room temperature, 30˚C and 40˚C. All the formulations were physically, chemically, and microbiologically stable. Conclusion: Mixed solvency concept has been successfully employed for enhancing the drug loading of poorly water soluble drug, cefixime. Keywords: Solubility, cefixime, liquisolid system, mixed solvency concept.

Aqueous Solubilization of Paclitaxel Using Hydrotropic Polymer Micelle

2007 ◽  
Vol 342-343 ◽  
pp. 421-424 ◽  
Author(s):  
Hyun Su Min ◽  
Hong Jae Lee ◽  
Sang Cheon Lee ◽  
Kyoung Hoon Kang ◽  
Jae Hwi Lee ◽  
...  
Keyword(s):  
Polymer Concentration ◽  
Aqueous Media ◽  
Water Soluble ◽  
Polymer Micelle ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poly Ethylene ◽  
Hydrotropic Agent ◽  
Poorly Water Soluble Drug

Hydrotropic block copolymers, consisting of a hydrophilic poly(ethylene glycol) (PEG) block and a hydrotropic polymer, poly(2-(4-(vinyl benzyloxy)-N,N-diethylnicotinamide)) [P(VBODENA)], block, were synthesized by atom transfer radical polymerization (ATRP) for aqueous solubilization of paclitaxel, a representative poorly water-soluble drug. These polymers showed an excellent solubilizing effect for paclitaxel in aqueous media in comparison with the corresponding hydrotropic agent and a control micelle (PEG-PLA) and such effect was significantly dependent on the polymer concentration and composition. Paclitaxel could be solubilized into polymer micelles in aqueous media without use of an organic solvent. Due to their promising properties such as micellar characteristics and hydrotropic solubilization, the hydrotropic polymer micelle system can be useful for formulation of paclitaxel and other poorly soluble drugs.

scholarly journals Amorphous Nanosuspensions Aggregated from Paclitaxel–Hemoglobulin Complexes with Enhanced Cytotoxicity

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 92
Author(s):  
Chao Qin ◽  
Xiaofei Xin ◽  
Xue Pei ◽  
Lifang Yin ◽  
Wei He
Keyword(s):  
Cancer Cells ◽  
High Efficiency ◽  
Drug Loading ◽  
Water Soluble ◽  
Rapid Release ◽  
Water Soluble Drug ◽  
Anti Cancer ◽  
Poorly Water Soluble ◽  
Cancer Agent ◽  
Poorly Water Soluble Drug

Amorphous nanosuspensions (ANSs) enable rapid release and improved delivery of a poorly water-soluble drug; however, their preparation is challenging. Here, using hemoglobin (Hb) as a carrier, ANSs aggregated from paclitaxel (PTX)–Hb complexes were prepared to improve delivery of the hydrophobic anti-cancer agent. An affinity study demonstrated strong interaction between Hb and PTX. Importantly, the complexes could aggregate into <300 nm ANSs with high drug loading, which acidic condition facilitated their formation. Furthermore, the ANSs possessed improved cytotoxicity against cancer cells over the crystalline nanosuspensions. Taken together, ANSs aggregated from PTX–Hb complexes were developed, which could kill cancer cells with high efficiency.

scholarly journals TECHNOLOGY DVELOPMENT FOR POLYMER MODIFICATION TO ENHANCE SOLUBILITY OF POORLY SOLUBLE DRUG

2018 ◽  
Vol 1 (1) ◽  
pp. 5-9
Author(s):  
Biresh Kumar Sarkar ◽  
Suraj Kumar Mishra ◽  
Suraj Kumar Mishra ◽  
Ajay Krishna Gupta ◽  
Shailendra S Solanki
Keyword(s):  
Dosage Form ◽  
Guar Gum ◽  
Water Soluble ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Polymer Modification ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solubilization of poorly soluble drugs is a frequently encountered challenge in screening studies of newchemical entities as well as in formulation design and development. Solubility of some drugs is very less; thesedrug molecules are often lipophilic and hence dissolution may be a problem in drug absorption from solid oraldosage forms. The increasing interest of the technology of dosage form with natural biopolymers has becomethe reason for undertaking present investigation on the possibility of modification of guar gum application inthe preparation of an oral solid dosage form of a poorly water soluble drug. Present study examines the effect ofmodified guar gum on the solubility of a poorly water-soluble Nevirapine. Modified guar gum was preparedusing heat treatment (110-120oC for 2 hours) method. It was characterized for viscosity and swelling index etc.The physical and co-grinding mixtures of Nevirapine with modified guar gum were prepared in 1:4 drugs togum ratio. The physical and co-grinding mixtures were characterized by DSC and FT-IR study. The studiesconfirmed that there was no interaction between drug and carrier. Prepared mixtures were evaluated forsolubility study and in vitro dissolution studies. The results of present investigation indicated that modified guargum can be a used for the development of oral dosage form with increased solubility and hence improveddissolution and oral bioavailability of poorly water soluble drug.

scholarly journals Formulation and development of fast dissolving oral film of a poorly soluble drug, frusemide with improved drug loading using mixed solvency concept and its evaluation

2018 ◽  
Vol 8 (6) ◽  
pp. 132-141 ◽  
Author(s):  
Garima Carpenter ◽  
R. K. Maheshwari
Keyword(s):  
Polyethylene Glycol ◽  
Sodium Benzoate ◽  
Sodium Citrate ◽  
Drug Loading ◽  
Research Work ◽  
Water Soluble ◽  
Polyethylene Glycol 200 ◽  
Poorly Soluble ◽  
Sodium Caprylate ◽  
Poorly Soluble Drug

The aim of the present research work is to explore the application of mixed solvency concept to formulate and develop a fast dissolving oral film of furosemide with improved drug loading. In the present study, poorly soluble drug, furosemide was tried to be solubilized by employing the combination of physiologically compatible water-soluble additives (solubilizers) to formulate its fast dissolving formulations. For the development of fast dissolving oral film, firstly, different film forming polymers were tested for their film properties. The second fast dissolving layer was also formed and optimized. Solubility studies were conducted to select water-soluble additives for formulation of fast dissolving drug layer. Keeping the total concentration less than 40 % w/v of mixed blends, different aqueous blends were prepared employing solubilizers from among sodium benzoate, sodium acetate, sodium citrate, urea, niacinamide, glycerin, propylene glycol, polyethylene glycol 200, polyethylene glycol 400, polyethylene glycol 600, and PVP K 30. Maximum solubility of furosemide was found in blends- F5 (10% sodium caprylate +2.5%sodium benzoate+ 2.5% niacinamide) and in blend F7 (10% sodium caprylate +2.5%sodium benzoate +2.5% sodium citrate + 2.5% niacinamide). Prepared films were evaluated for drug content, thickness, folding endurance, tensile strength and hydration ratio. Keywords: Furosemide, fast dissolving oral film, mixed solvency concept.

Poorly Water Soluble Drug Nanostructures via Surface Solvent Evaporation

Nano LIFE ◽  
2015 ◽  
Vol 05 (03) ◽  
pp. 1540005 ◽  
Author(s):  
Michael Graham ◽  
Yonghong Yang ◽  
Aled D Roberts ◽  
Haifei Zhang
Keyword(s):  
Solvent Evaporation ◽  
Water Soluble ◽  
Aluminum Surface ◽  
X Ray Diffraction ◽  
Nanoparticle Suspension ◽  
Water Soluble Drug ◽  
Drug Compounds ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

A high percentage of developed drug compounds are poorly soluble in water, which severely limits their applications. Nanotechnology has been used to address this issue. Here we describe a simple and versatile bottom-up approach for the preparation of drug nanostructures by surface solvent evaporation on aluminum surface and polymer-coated surface. Three poorly water soluble drug compounds, including griseofulvin (GF), curcumin and antimalarial compound SL-2-25 have been investigated as model compounds. The structures are mainly characterized by scanning electronic microscopy (SEM) while the GF nanoparticles are also examined by powder X-ray diffraction (PXRD) and thermogravimetric analysis (TGA). A variety of structures including microassemblies composed of nanoparticles, nanospheres and nanofibers have been produced. A sonication method can be employed to produce aqueous nanoparticle suspension.

scholarly journals Formulating a poorly water soluble drug into an oral solution suitable for paediatric patients; lorazepam as a model drug

2017 ◽  
Vol 100 ◽  
pp. 205-210 ◽  
Author(s):  
A.C. van der Vossen ◽  
I. van der Velde ◽  
O.S.N.M. Smeets ◽  
D.J. Postma ◽  
M. Eckhardt ◽  
...  
Keyword(s):  
Oral Solution ◽  
Water Soluble ◽  
Paediatric Patients ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Model Drug ◽  
Poorly Water Soluble Drug

scholarly journals Formulation and development of vaginal films of poorly water soluble drug, metronidazole, using mixed solvency concept and their evaluations

2018 ◽  
Vol 8 (6) ◽  
pp. 41-48 ◽  
Author(s):  
Neha Gahlot ◽  
Rajesh Kumar Maheshwari
Keyword(s):  
Dosage Form ◽  
Research Work ◽  
Cost Effective ◽  
Stability Study ◽  
Water Soluble ◽  
High Concentration ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Aim: To deliver antibacterial therapy in an efficacious way, film dosage form has been proposed for drug delivery in vagina which can overcome bioavailability issues of poorly water soluble drugs. The present research work is aimed to explore the application of mixed solvency concept to increase solubility of poorly water soluble drug, metronidazole. Materials and Methods: Metronidazole, a slightly soluble drug in water was tried to be solubilized by employing the combination of solubilizers like niacinamide, sodium benzoate, sodium caprylate, caffeine and urea to endeavour its fast dissolving film formulations. The procured sample of drug was characterized by UV, IR and DSC studies. The formulations were evaluated for various properties of film such as thickness, folding endurance, surface pH, disintegration time and thin layer chromatography. Stability studies of vaginal films of metronidazole were performed for ten weeks at room temperature, and refrigerated conditions. Results and Discussion: It was found that 97.54% and 97.58% of drug was remaining after stability study at respective temperatures in batch F1 and 98.53% and 96.57% in batch F4.Conclusion: It was concluded that the approach of mixed solvency concept is novel, safe, cost-effective and user friendly. It also eliminates the problem of toxicity associated with high concentration of water-soluble solubilizers. So, it may be employed in dosage form development of drugs with poor solubility to overcome bioavailability issues. Keywords: Solubility, metronidazole, vaginal films, mixed solvency concept.

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