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Drug Delivery Systems for the Controlled Delivery of Berberine
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Rosario Pignatello, Simona Cianciolo, Agata K. Giuffrida
In another work, BER powder was previously dispersed in a melted glyceryl behenate solution and then submitted to high pressure homogenization (HPH). A homogeneous population of SLN was obtained with a mean size nearby 150 nm and a spherical shape, with a net negative Zeta potential value (around −19 mV).
Nanocarrier Technologies for Enhancing the Solubility and Dissolution Rate of Api
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Ashwini Deshpande, Tulshidas S. Patil
These are biocompatible, biodegradable lipids which are solid at room and body temperature. The lipids can be used within the range of 5–40%. Examples include: Triglycerides (trimyristin, tripalmitin, tristearin).Polymers like soya phosphatidyl choline, PLGA, sodium alginate, chitosan, etc.Glyceryl monostearate (GMS) (Imwitor® 900).Glyceryl behenate (Compritol® 888 ATO, GeleolTM).Glyceryl palmitostearate (Precirol® ATO 5).Wax (cetyl palmitate).
Organic Nanocarriers for Brain Drug Delivery
Published in Carla Vitorino, Andreia Jorge, Alberto Pais, Nanoparticles for Brain Drug Delivery, 2021
Marlene Lúcio, Carla M. Lopes, Eduarda Fernandes, Hugo Gonẹalves, Maria Elisabete C. D. Real Oliveira
Cryptococcus neoformans-mediated meningoencephalitis is a severe infection of the human CNS. The poor penetration of therapeutic agents across the BBB limits the efficiency of available treatments. Therefore, Du et al. [184] evaluated the potential of NLCs as nose-to-brain carriers for treating meningoencephalitis [184]. The authors used Miglyol® 812 (caprylic/capric triglycerides) as a liquid lipid, glyceryl behenate as a solid lipid and Tween® 80 and Solutol HS 15 (a permeability enhancer) as surfactant agents. Firstly, fluorescent-dye-loaded NLCs were prepared to investigate their uptake into the cytoplasm of C. neoformans cells. The results suggested that NLCs present excellent penetration ability into the thick capsule structure of C. neoformans. The authors also prepared ketoconazole (keto)-loaded NLCs with the following properties: average particle size of 102.1 ± 0.44 nm; PDI of 0.195 ± 0.005, indicating a homogeneous particle size distribution; average zeta potential of -2.1 ± 0.18 mV; EE of 70.4% ± 3.4%; and good stability over two weeks. In vitro studies revealed that keto-loaded NLCs had higher antifungal activity, with a cell inhibition rate fourfold higher than the free drug, even at low concentrations. Animal imaging analysis demonstrated that NLCs can enter brain tissues via the olfactory bulbs after i.n. administration, bypassing the BBB, as well as that the NLCs remained in tissue for longer periods. Moreover, i.n.-administrated keto-NLCs significantly inhibited cerebral C. neoformans colonisation and proliferation in mouse brain tissue when compared to free keto.
M6P-modified solid lipid nanoparticles loaded with matrine for the treatment of fibrotic liver
Published in Drug Delivery, 2023
Xiaochuan Tan, Yumei Hao, Nai Ma, Yige Yang, Wenzhen Jin, Ya Meng, Chuchu Zhou, Wensheng Zheng, Yujia Zhang
Glyceryl monostearate and stearic acid were purchased from Beijing Fengli Jingqiu Commerce and Trade Co., Ltd (Beijing, China). Glyceryl behenate was purchased from Guangzhou Tianrun Pharmaceutical Co., Ltd (Guangzhou, China). Egg yolk lecithin and soybean lecithin were purchased from Shanghai Tywei Co., Ltd (Shanghai, China). Poloxamer 188, Span 85, Tween 80, glycerin, and Brij S10 were obtained from Sigma-Aldrich (ST. Louis, USA). MT and FBS was purchased from Innochem Technology Co., Ltd (Beijing, China). P-nitrophenyl-a-D-mannopyranoside, N-succinimidyl-S-acetylthioacetate (SATA), and phosphatidylethanolamine-PEG-maleimide (DSPE-PEG-MAL) were bought from Shanghai Yiyan Biological Technology Co., Ltd (Shanghai, China). Human serum albumin was purchased from Tokyo Chemical Industry (Shanghai) Development Co., Ltd (Shanghai, China). Phosphorus oxychloride, palladium 10% on carbon, and thiophosgen were bought from Energy Chemical Technology (Shanghai) Co., Ltd (Shanghai, China). Dialysis bags (2500 kDa cutoff) were purchased from Shanghai Yuanye Biological Technology Co., Ltd (Shanghai, China). Ultrafiltration tubes (3 kDa cutoff) were bought from Merck Millipore (Germany). Acetonitrile, methanol, ethanol, and ethyl acetate were of HPLC grade, and other reagents were of analytical grade.
Preparation and optimization of glyceryl behenate-based highly porous pellets containing cilostazol
Published in Pharmaceutical Development and Technology, 2018
Kyu-Mok Hwang, Woojin Byun, Cheol-Hee Cho, Eun-Seok Park
Glyceryl behenate is a mixture of glycerol esters and behenic acid11. It has a waxy texture and was originally introduced as a lubricant in tablets12. The good compressibility13 and molecular binding force properties of glyceryl behenate make it useful as a release retardant in sustained-release dosage forms. Since it is a lipid, its density is low enough to float on water14. Some studies reported that postcompression thermal treatment, or sintering, of a glyceryl behenate-based matrix at high temperature led to a slower release rate15,16. This effect is thought to be caused by redistribution of melted lipid, which increased the matrix integrity. Unfortunately, the thermal treatment was only implemented at a temperature above the melting point of the lipid and the sintering effect at a temperature near its melting point remains unclear.
Development of sustained release gastro-retentive tablet formulation of nicardipine hydrochloride using quality by design (QbD) approach
Published in Drug Development and Industrial Pharmacy, 2018
Vijay S. Chudiwal, Sadhana Shahi, Swapnil Chudiwal
The mathematical relationship of factors coefficients and corresponding P values for the responses obtained via regression analysis are presented in Table 9. Factors having P values less than .05 were considered as significant. The results obtained from the Box–Behnken design (Table 9) revealed that Y1 was significantly affected by X1: Glyceryl behenate (mg/tab) and X2: HPMC K15M (mg/tab) (p < .05). From the effects, it can be concluded that X1: Glyceryl behenate (mg/tab) was the most influencing factor affecting negatively for entire drug release from tablet dosage form. The same can be confirmed from the main effect plots for drug release (%) (Y1) Q1.5, Q8 and Q24. Conversely, the amount of HPMC K15M positively affected the drug release (%) (Y1) Q1.5, Q8 and Q24 (Figure 4(a–c)). The effect of the three studied factors was also investigated on Y2. In Table 9, it was observed that Y2 was significantly affected by X3: Sodium bicarbonate (mg/tab) (p < .05) (Figure 4(d)). As learned from regression analysis, X3: Sodium bicarbonate (mg/tab) gain was inversely correlated with Y2 (p < .05) (Table 9).