Sustained Ocular Drug Delivery Utilizing Dendrimer-Based Hydrogels.

Sustained ocular drug delivery utilizing dendrimer-based hydrogels.

Filed under: Drug and Alcohol Rehabilitation

Nanomedicine (Lond). 2012 Dec; 7(12): 1800
Zeng X, Zhang Y, Sand A, Nyström AM

HubMed – drug

 

[Neurodegeneration in multiple sclerosis and the neuroprotective effect of glatiramer acetate: a literature review].

Filed under: Drug and Alcohol Rehabilitation

Zh Nevrol Psikhiatr Im S S Korsakova. 2012; 112(9 Pt 2): 123-8

The two-phase model of the pathogenesis of multiple sclerosis (MS) is discussed in the aspect of inflammation and neurodegeneration processes. In the first phase, there are inflammation processes with frequent exacerbations and remissions and multiple lesions on MRI. An axonal lesion (neurodegeneration) is seen in this stage, even in the very beginning, i.e. in the stage of clinically isolated syndrome. The possibilities of treatment of neurodegenerative changes, in particular, with glatiramer acetate (GA) or copaxon, are reviewed. Copaxon induces a switch from Th1-cells to GA-specific Th2-lymphocyte production which can produce neurotrophic factors. Clinical and MRI data as well as experimental results supporting the neuroprotective effect of this drug are presented.
HubMed – drug

 

Design and development of controlled porosity osmotic tablet of diltiazem hydrochloride.

Filed under: Drug and Alcohol Rehabilitation

J Adv Pharm Technol Res. 2012 Oct; 3(4): 229-36
Shahi SR, Zadbuke NS, Gulecha B, Shivanikar SS, Shinde SB

The present work aims towards the design and development of extended release formulation of freely water-soluble drug diltiazem hydrochloride (DLTZ) based on osmotic technology by using controlled porosity approach. DLTZ is an ideal candidate for a zero-order drug delivery system because it is freely water-soluble and has a short half-life (2-3 h). Sodium chloride (Osmogen) was added to the core tablet to alter the solubility of DLTZ in an aqueous medium. Cellulose acetate (CA) and sorbitol were used as semipermeable membrane and pore former, respectively. The effect of different formulation variables namely concentration of osmogen in the core tablet, % pore former, % weight gain, pH of the dissolution medium and agitation intensity on the in vitro release was studied. DLTZ release was directly proportional to % pore former and inversely proportional to % weight gain. The optimized formulation (F8) delivered DLTZ independent of pH and agitation intensity for 12 h at the upper level concentration of % pore former (25% w/w) and middle level concentration of % weight gain (6% w/w). The comparative study of elementary osmotic pump (EOP) and controlled porosity osmotic pump revealed that it superior than conventional EOP and also easier and cost effective to formulate.
HubMed – drug

 

Terpenes: Effect of lipophilicity in enhancing transdermal delivery of alfuzosin hydrochloride.

Filed under: Drug and Alcohol Rehabilitation

J Adv Pharm Technol Res. 2012 Oct; 3(4): 216-23
Prasanthi D, Lakshmi PK

Transdermal drug delivery has attracted much attention as an alternative to intravenous and oral methods of delivery. But the main barrier is stratum corneum. Terpenes classes of chemical enhancers are used in transdermal formulations for facilitating penetration of drugs. The aim of the study is to evaluate terpenes as skin penetration enhancers and correlate its relationship with permeation and lipophilicity. In this study, alfuzosin hydrochloride (AH) hydrogels were prepared with terpenes using Taguchi orthogonal array experimental design. The formulations contained one of eight terpenes, based on their lipophilicity (log P 2.13-5.36). The percutaneous permeation was studied in rat skin using diffusion cell technique. Flux, cumulative amount, lag time and skin content of AH were measured over 24 hours and compared with control gels. Nerolidol with highest lipophilicity (log P 5.36 ± 0.38) showed highest cumulative amount (Q(24)) of 647.29 ± 18.76 ?g/cm(2) and fluxrateof 28.16 ± 0.64 ?g/cm(2)/hour. It showed decreased lag time of 0.76 ± 0.15 hours. Fenchone (2.5%) (log P 2.13 ± 0.30) produced the longest lag time 4.8 ± 0.20 hours. The rank order of enhancement effect was shown as nerolidol > farnesol > limonene > linalool > geraniol > carvone > fenchone > menthol. Lowest skin content was seen with carvone. Increase in lipophilicity of terpenes showed increase in flux, cumulative amount (Q(24)), and enhancement ratio which was significant with P < 0.000. But lag time was decreased and no correlation was found between lipophilicity and skin content. Histological studies showed changes in dermis which can be attributed to disruption of lipid packing of stratum corneum due to effect of nerolidol within lipid lamellae. It was found that small alcoholic terpenes with high degree of unsaturation enhance permeation of hydrophilic drugs, liquid terpenes enhance better than solid terpenes and terpenes with high lipophilicity are good penetration enhancers. HubMed – drug

 

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