Preparation and Biological Evaluation of Silybin Liposomes for the Treatment of Liver Disorders

Aim: The aim of the present study was to develop silybin liposome by incorporating phosphatidyl choline & cholesterol so as to increase its oral bioavailability and liver targeted enhanced hepatoprotection. Methodology: Thin film hydration technique was used for the development of liposomes by using phosphatidyl choline, cholesterol and drug. Liposomes were evaluated for vesicle size, zeta potential, PDI, encapsulation efficiency, surface morphology and in vitro drug release study. Further the optimized formulation was evaluated for APAP-induced alterations in liver and kidney function tests in rats and histopathological studies. Results: The results were promising with a sustained drug release of 80% within 20hrs, optimized vesicle size of 276nm and 89% encapsulation efficiency. The animal studies demonstrated superior hepatoprotective effect compared to silybin solution. Conclusion: The silybin liposomes showed better in-vitro release & in-vivo hepatoprotection along with better animal activity & improvement in histopathological changes as compared to silybin.

Lipodystrophy of Abdominal Pannus: A Severe Complication of Phosphatidyl Choline Injections

Abstract“Injection lipolysis” or “mesotherapy” is done for introducing various substances into deeper layers of the skin with the aim to dissolve subcutaneous fat. However, the safety profile of these chemicals is poorly regulated. Therefore, they may cause side effects or long-term sequelae that can be disastrous for the patient. We present such a case that required surgical management to salvage it and to give an aesthetically acceptable result.

In Vitro Dissolution Evidence for Sustained and Prolonged Release of Vitamin C in a Phosphatidyl Choline-Enriched Lipid Encapsulation

Objectives In vitro dissolution tests are valuable first-step tools in the development of bioavailable delivery systems, making it possible to assess the performance of novel technologies in releasing active ingredients through the amount dissolved in a dissolution medium. The objective of this study was to evaluate whether phosphatidyl choline-enriched lipid encapsulation releases the majority of vitamin C as ascorbic acid past the stomach in a standard in vitro dissolution procedure and to assess the release profile. Methods A novel phosphatidyl choline-enriched lipid encapsulation that is solid at room temperature was tested for dissolution in a standard dissolution apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. One serving (included 1000 mg ascorbic acid) was placed into vessels containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.8) for an additional 360 minutes. Aliquots were tested for ascorbic acid concentration at 8 time points by titration. The data was compared with 1000 mg of regular ascorbic acid in a capsule format. Results The phosphatidyl choline-enriched lipid encapsulation released 36% of the vitamin C at 2 hours in the acid phase and released 56% at 3 hours, 67% at 4 hours, 85% at 6 hours and 98% at 8 hours in the intestinal phase. Regular vitamin C filled capsules released 100% of the vitamin C at 30 minutes. Conclusions The dissolution results indicated that phosphatidyl choline-enriched lipid encapsulation can pass the stomach and release the majority of vitamin C in the small intestine. The encapsulation demonstrated a sustained and prolonged release of vitamin C over an 8 hour period. The release profile observed in this in vitro study suggests phosphatidyl choline-enriched lipid encapsulation may improve nutrient absorption and bioavailability which requires further testing including human clinical trials. Funding Sources This study was supported by Lonza (Greenwood, SC) and Ritual (Natals Inc, Los Angeles, CA).

Hyaluronic acid–lipid binding

Background Phospholipid (PL)–hyaluronic acid (HA) interactions are relevant to aging-associated vitreous humor liquefaction, therapies for dry eye disease, skin-care products and synovial joint lubrication. Phosphatidyl choline–HA interactions have been well characterized. However, other major lipids found in tears, vitreous humor and synovial joints have not. The purpose of this study was to bridge this gap of knowledge. Methods HA (1600 kDa) at 5 mg/mL, was mixed with various lipids ranging in concentration from 0.1 to 10 mg/mL in D2O. HA–PL binding was measured from the decrease in HA proton resonance intensity with binding using a nuclear magnetic resonance spectrometer. Results Cholesterol weakly bound to HA, followed by monoglyceride and palmitoyl palmitate < phosphatidyl choline, phosphatidic acid and sphingomyelin. The maximum amount of PL bound was 14 ± 1 µmoles inferring a 1 to 1 molar ratio of bound PL to HA dimer. Monoglyceride and palmitoyl palmitate required two to three times more lipid to achieve 100% bound HA compared to PL. Conclusions Physiological levels of HA, phosphatidyl choline and sphingomyelin would result in only 4% of the hydrophobic hydrogens of HA to be bound. HA–PL binding interactions could be important for therapeutic use of HA in eye drops in future studies to treat dry eye and to trap PL entering the VH to keep them from forming light scattering micelles. HA–lipid binding may also be relevant to the therapeutic effects of topical skin-care products. Both head group and hydrocarbon chain moieties influence HA–lipid interactions.

Choline Phosphate Lipid Insert and Rigidify Cell Membrane for Targeted Cancer Chemo-immunotherapy

To prevent tumor reproduction and metastasis, a method to modify the membrane of cancer cells was designed to suppress their vitality. We synthesized a phosphatidyl choline reversed choline phosphate lipid...

The Effect of Curcumin in Patients with Chronic Fatigue Syndrome (or) Myalgic Encephalomyelitis Disparate Responses in Different Disease Severities

Myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS), is a chronic and often disabling disease. Although the exact pathophysiological mechanism of ME/CFS is unknown, immunological abnormalities may play an important role. Curcumin is an herb with powerful anti-oxidative and anti-inflammatory properties. Therefore, we hypothesized that curcumin would have favorable effects on symptomatology in ME/CFS patients. In an open trial among 65 ME/CFS participants, 6 stopped the use of curcumin because of side effects and 8 did not complete the end of study questionnaire. Before and 8 weeks after the use of curcumin complexed with phosphatidyl choline-, 500 mg bid, participants completed the CDC inventory for assessment of Chronic Fatigue Syndrome. The CDC questions (n=19) were scored and divided into 2 parts: the first being specific for CFS complaints (n=9), the second being scores of less specific symptoms (n=10); denoted as CDC other score. Results showed that 8 weeks of curcumin significantly decreased the CDC CFS-related symptom scores and CDC other scores, especially in patients with mild disease. Conclusion: in this open-labeled study 8 week curcumin use in a phosphatidyl choline complex reduced ME/CFS symptomatology, especially in patients with mild disease severity.

Development of Novel, Potent Phosphatidyl–Choline-Specific Phospholipase C Inhibitors

The phosphatidyl–choline-specific phospholipase C (PC-PLC) enzyme has been shown to be an important enzyme involved in various cell-signaling processes. Furthermore, PC-PLC has been shown to be upregulated in various cancer cell lines, thereby presenting itself as a potential anti-cancer therapeutic target. Current PC-PLC inhibitors, including the literature standard inhibitor D609 possess characteristics making them unsuitable for clinical use. We have discovered a new class of potent PC-PLC inhibitors with much improved activity and drug-like properties than D609. The synthesis and SAR study of this class of active compounds is presented.

Daya Hidup Spermatozoa Sapi Limousin yang Dipreservasi dengan Pengencer Tris dan Berbagai Konsentrasi Sari Kedelai

ABSTRAK digunakan sebagai salah satu bahan pengencer semen pengganti kuning telur ayam. Penelitian ini bertujuan untuk menguji pengaruh sari kedelai dalam pengencer Tris terhadap motilitas dan daya hidup spermatozoa sapi limousin yang dipreservasi pada suhu 5oC. Semen ditampung dengan vagina buatan. Semen segar yang memenuhisyarat dibagi kedalam empat buah tabung reaksi yang masing-masing berisi pengencer perlakuan, yakni: 80% pengencer dasar Tris + 20% kuning telur (Tris), 97% pengencer dasar Tris + 3% sari kedelai (SK3), 95% pengencer dasar Tris + 5% sari kedelai (SK5), dan 93% pengencer dasar Tris + 7% sari kedelai (SK7). Semen yang telah diencerkan disimpan di dalam refrigerator pada suhu 5oC, dan dievaluasi motilitas dan viabilitas spermatozoa setiap hari hingga hari kelima. Hasil penelitian menunjukkan bahwa motilitas dan viabilitas spermatozoa di dalam pengencer Tris nyata (P<0,05) lebih tinggi dibandingkan dengan spermatozoa di dalam pengencer SK3, SK5, dan SK7 selama empat hari penyimpanan. Berdasarkaan hasil penelitian dapat disimpulkan bahwa pengencer Tris-kuning telur lebih baik dalam mempertahankan motilitas dan daya hidup spermatozoa sapi limousin dibandingkan dengan pengencer Tris-sari kedelai yang dipreservasi pada suhu 5°C. Pengencer Tris dengan konsentrasi 3% sari kedelai lebih baik dibandingkan dengan konsentrasi 5% dan 7%.Kata Kunci : sapi limousine, sari kedelai, semen, trisABSTRACTSoybean contains anlecithin (phosphatidyl choline), that has the potential to be used as substitute for chicken egg yolk as one of the semen extender compound. The aim of this research was to examine the effect of soybean juice in Tris extender on the motility and viability of Limousin cattle spermatozoa preserved at 5oC. Semen was collected using artificial vagina. Fresh semen was divided into four tubes containing a treatment extender, i.e. 80% Tris base extender + 20 egg yolk (Tris), 97% Tris-based extender + 3% soybean juice (SJ3), 95% Tris-based extender + 5% soybean juice (SJ5), 93% Tris-based extender + 7% soybean juice (SJ7), respectively. Diluted-semen was preserved in refrigerator at 5oC, and evaluation of spermatozoa motility and viability were conducted on daily basis up to five days. The result showed that percentages of motility and viability of spermatozoa in Tris-yolk extender were significantly (P<0.05) higher than spermatozoa in SJ3, SJ5, and SJ7extenders during four days of storage. In conclusion, Tris-yolk extender is better than Tris-soybean juice in maintaining the spermatozoa motility and viability of Limousin cattle preserved at 5°C. Tris extender containing 3% soybean juice is better than 5% and 7%.Keywords: limousin cattle, semen, soybean juice, tris