Displaying publications 21 - 40 of 48 in total

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  1. Swelling behaviour and controlled drug release from cross-linked κ-carrageenan/NaCMC hydrogel by diffusion mechanism
    Hezaveh H, Muhamad II, Noshadi I, Shu Fen L, Ngadi N
    J Microencapsul, 2012;29(4):368-79.
    PMID: 22309480 DOI: 10.3109/02652048.2011.651501
    We studied a model system of controlled drug release using beta-carotene and κ-carrageenan/NaCMC hydrogel as a drug and a device, respectively. Different concentrations of genipin were added to crosslink the beta-carotene loaded beads by using the dripping method. Results have shown that the cross-linked beads possess lower swelling ability in all pH conditions (pH 1.2 and 7.4), and swelling ratio decreases with increasing genipin concentration. Microstructure study shows that cross-linking has enhanced the stability and structure of the beads network. Determination of diffusion coefficient for the release of encapsulated beta-carotene indicates less diffusivity when beads are cross-linked. Swelling models using adaptive neuro fuzzy show that using genipin as a cross-linker in the kC/NaCMC hydrogels affects the transport mechanism. The model shows very good agreement with the experimental data that indicates that applying ANFIS modelling is an accurate, rapid and simple way to model in such a case for controlled release applications.
    Matched MeSH terms: Drug Compounding/methods*
  2. Sodium carboxymethyl cellulose hydrogels containing reduced graphene oxide (rGO) as a functional antibiofilm wound dressing
    Ali NH, Amin MCIM, Ng SF
    J Biomater Sci Polym Ed, 2019 06;30(8):629-645.
    PMID: 30896336 DOI: 10.1080/09205063.2019.1595892
    Biofilms comprise bacteria attached to wound surfaces and are major contributors to non-healing wounds. It was found that the increased resistance of biofilms to antibiotics allows wound infections to persist chronically in spite of antibiotic therapy. In this study, the reduced form of graphene oxide (rGO) was explored as plausible antibiofilm agents. The rGO was synthesized via reducing the functional groups of GO. Then, rGO were characterized using zetasizer, X-ray photoelectron spectroscopy, UV-Vis spectroscopy and FESEM. The rGO were then formulated into sodium carboxymethyl cellulose (NaCMC) hydrogels to form rGO hydrogel and tested for antibiofilm activities in vitro using XTT test, and in vivo biofilm formation assay using nematodes C. elegans. Reduced GO hydrogel was successfully formed by reducing the functional groups of GO, and a reduction of up to 95% of functional groups was confirmed with X-ray photoelectron spectroscopy analysis. XTT tests confirmed that rGO hydrogels reduced biofilm formation by S. aureus (81-84%) and P. aeruginosa (50-62%). Fluorescence intensity also confirmed that rGO hydrogel can inhibit biofilm bacteria in C. elegans experiments. This study implied that rGO hydrogel is an effective antibiofilm agent for infected wounds.
    Matched MeSH terms: Drug Compounding/methods
  3. Development and Standardization of Moringa oleifera Leaves as a Natural Dietary Supplement
    Ali MA, Yusof YA, Chin NL, Ibrahim MN, Muneer S
    J Diet Suppl, 2019;16(1):66-85.
    PMID: 29469600 DOI: 10.1080/19390211.2018.1429517
    Moringa oleifera leaves were selected as a model due to their hundreds of health benefits. On the other hand, the powder of these leaves has exhibited poor flowability, low tensile strength, bitter taste, poor dissolution rate, and lack of information regarding dosage. These are the common hurdles and limitations in the adaptation of herbal-based medications. Therefore, a comprehensive study was planned to introduce herbal-based medicines into mainstream medicines by standardization according to the U.S. Food and Drug Administration (FDA) and international pharmaceutical standards. A Simplex Lattice Design (SLD) of Design Expert 8.0 software was used to formulate different concentrations of superdisintegrant, binder/diluent, and sweeteners. An Instron Universal Testing machine coupled with a 13 mm stainless cylindrical die was used to manufacture tablets by means of direct compression method at 20 kN applied force. Therefore, selection of excipients was made on the basis of their tensile strength, flowability, and taste-masking properties. Optimum formulation was tested on rabbits for toxicity and growth rate. All formulated tablets were evaluated on standard parameters for orally disintegrating tablets described by the Food and Drug Authority (U.S.). The optimum formulation fulfills all standard parameters such as hardness, disintegration time, friability, and dissolution rate. The present formulation showed no toxicity when tested on rabbits. The present study provides a fundamental understanding of the tableting characteristics of natural medicines. The present study provides information that will help to overcome the challenges.
    Matched MeSH terms: Drug Compounding/methods*
  4. Microencapsulation of alginate-immobilized bagasse with Lactobacillus rhamnosus NRRL 442: enhancement of survivability and thermotolerance
    Shaharuddin S, Muhamad II
    Carbohydr Polym, 2015 Mar 30;119:173-81.
    PMID: 25563958 DOI: 10.1016/j.carbpol.2014.11.045
    The aim of this research was to enhance the survivability of Lactobacillus rhamnosus NRRL 442 against heat exposure via a combination of immobilization and microencapsulation processes using sugarcane bagasse (SB) and sodium alginate (NaA), respectively. The microcapsules were synthesized using different alginate concentration of 1, 2 and 3% and NaA:SB ratio of 1:0, 1:1 and 1:1.5. This beneficial step of probiotic immobilization before microencapsulation significantly enhanced microencapsulation efficiency and cell survivability after heat exposure of 90°C for 30s. Interestingly, the microcapsule of SB-immobilized probiotic could obtain protection from heat using microencapsulation of NaA concentration as low as 1%. SEM images illustrated the incorporation of immobilized L. rhamnosus within alginate matrices and its changes after heat exposure. FTIR spectra confirmed the change in functional bonding in the presence of sugarcane bagasse, probiotic and alginate. The results demonstrated a great potential in the synthesis of heat resistant microcapsules for probiotic.
    Matched MeSH terms: Drug Compounding/methods*
  5. Influence of beta-cyclodextrin and chitosan in the formulation of a colon-specific drug delivery system
    Rehman K, Amin MC, Muda S
    Drug Res (Stuttg), 2013 Dec;63(12):657-62.
    PMID: 23842943 DOI: 10.1055/s-0033-1349129
    The increase in diseases of the colon underscores the need to develop cost-effective site-directed therapies. We formulated a polysaccharide-based matrix system that could release ibuprofen under conditions simulating those in the colon by employing a wet granulation method. Tablets were prepared in a series of formulations containing a polysaccharide (beta-cyclodextrin and chitosan) matrix system along with ethylcellulose. We characterized physicochemical properties and performed an in vitro drug release assay in the absence and presence of digestive enzymes to assess the ability of the polysaccharides to function as a protective barrier against the upper gastrointestinal environment. Fourier transform infrared spectroscopy studies revealed no chemical interaction between ibuprofen and polysaccharides; however, spectrum analysis suggested the formation of an inclusion complex of beta-cyclodextrin with ibuprofen. The formulations contained 50% ethylcellulose and 50% beta-cyclodextrins (1:1) were proven to be the better formulation that slowly released the drug until 24 h (101.04 ± 0.65% maximum drug release in which 83.08 ± 0.89% drug was released in colonic medium) showed better drug release profiles than the formulations containing chitosan. We conclude that a beta-cyclodextrin drug carrier system may represent an effective approach for treatment of diseases of the colon.
    Matched MeSH terms: Drug Compounding/methods
  6. Tableting Properties and Compression Models of Labisia pumila Tablets
    Etti CJ, Yusof YA, Chin NL, Mohd Tahir S
    J Diet Suppl, 2017 Mar 04;14(2):132-145.
    PMID: 27487244
    The tableting properties of Labisia pumila herbal powder, which is well known for its therapeutic benefits was investigated. The herbal powder was compressed into tablets using a stainless steel cylindrical uniaxial die of 13-mm- diameter with compaction pressures ranging from 7 to 25 MPa. Two feed weights, 0.5 and 1.0 g were used to form tablets. Some empirical models were used to describe the compressibility behavior of Labisia pumila tablets. The strength and density of tablets increased with increase in compaction pressure and resulted in reduction in porosity of the tablets. Smaller feeds, higher forces and increase in compaction pressure, contributed to more coherent tablets. These findings can be used to enhance the approach and understanding of tableting properties of Labisia pumila herbal powder tablets.
    Matched MeSH terms: Drug Compounding/methods*
  7. Microencapsulation of alpha-mangostin into PLGA microspheres and optimization using response surface methodology intended for pulmonary delivery
    Elsaid Ali AA, Taher M, Mohamed F
    J Microencapsul, 2013;30(8):728-40.
    PMID: 23631380 DOI: 10.3109/02652048.2013.788081
    Documented to exhibit cytotoxicity and poor oral bioavailability, alpha-mangostin was encapsulated into PLGA microspheres with optimization of formulation using response surface methodology. Mixed levels of four factors Face central composite design was employed to evaluate critical formulation variables. With 30 runs, optimized formula was 1% w/v polyvinyl alcohol, 1:10 ratio of oil to aqueous and sonicated at 2 and 5 min time for primary and secondary emulsion, respectively. Optimized responses for encapsulation efficiency, particle size and polydispersity index were found to be 39.12 ± 0.01%, 2.06 ± 0.017 µm and 0.95 ± 0.009, respectively, which matched values predicted by mathematical models. About 44.4% of the encapsulated alpha-mangostin was released over 4 weeks. Thermal analysis of the microspheres showed physical conversion of alpha-mangostin from crystallinity to amorphous with encapsulated one had lower in vitro cytotoxicity than free alpha-mangostin. Aerodynamic diameter (784.3 ± 7.5 nm) of this alpha-mangostin microsphere suggests suitability for peripheral pulmonary delivery.
    Matched MeSH terms: Drug Compounding/methods
  8. Stomach-site specific drug delivery system of clarithromycin for eradication of Helicobacter pylori
    Rajinikanth PS, Mishra B
    Chem Pharm Bull (Tokyo), 2009 Oct;57(10):1068-75.
    PMID: 19801860
    Gellan gum based floating beads containing clarithromycin (FBC) were prepared by iontotropic gelation method for stomach-specific drug delivery against Helicobacter pylori. The scanning electron microscope photograph indicated that prepared beads were spherical in shape with rough outer surface. Formulation variables such as concentrations of gellan, calcium carbonate and drug loading influenced the in vitro drug release characteristics of prepared beads. In vitro release rate of clarithromycin was corrected using first order degradation rate constant which is degraded significantly during the release study in simulated gastric fluid pH 2.0. Further, the absence of interactions between drug and polymer was confirmed by differential scanning calorimetry analysis. Kinetic treatment of the in vitro drug release data with different kinetic equations revealed matrix diffusion mechanism. Prepared beads showed good anti-microbial activity against isolated H. pylori strain. The prepared beads have shown good in vivo floating efficiency in rabbit stomach. The stability studies of beads did not show any significant changes after storage of beads at 40 degrees C/75% relative humidity for 6 months. The preliminary results from this study suggest that floating beads of gellan can be used to incorporate antibiotics like clarithromycin and may be effective when administered locally in the stomach against H. pylori.
    Matched MeSH terms: Drug Compounding/methods*
  9. Challenges in pediatric drug use: A pharmacist point of view
    Balan S, Hassali MA, Mak VSL
    Res Social Adm Pharm, 2017 May-Jun;13(3):653-655.
    PMID: 27493130 DOI: 10.1016/j.sapharm.2016.06.014
    The pediatric population is an enormously diverse segment of population varying both in size and age. The diversity caused pharmacists face various challenges primarily related to procuring, provision as well as use of drugs in this group of patients. Pediatric dose calculation is particularly a concern for pharmacists. Another challenge faced by pharmacists is unavailability of suitable formulations for pediatric use. This has also led many pharmacists to prepare extemporaneous liquid preparations, even though stability data on such preparations are scarce. Some extemporaneous preparations contain excipients which are potentially harmful in children. Besides that, inadequate labeling and drug information for pediatric drug use had not only challenged pharmacists in recommending and optimizing drug use in children, but also inadvertently caused many drugs used outside the approved terms of the product license (off-label use). Pharmacists are striving to stay connected to overcome the common and comparable challenges faced in their day to day duties and strive to maximize the safe and effective use of medicines for children.
    Matched MeSH terms: Drug Compounding/methods*
  10. Development of a novel direct compressible co-processed excipient and its application for formulation of Mirtazapine orally disintegrating tablets
    Loke YH, Chew YL, Janakiraman AK, Lee SK, Uddin ABMH, Goh CF, et al.
    Drug Dev Ind Pharm, 2024 Jan;50(1):36-44.
    PMID: 38149637 DOI: 10.1080/03639045.2023.2294095
    INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited.

    OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs.

    METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation.

    RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min.

    CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.

    Matched MeSH terms: Drug Compounding/methods
  11. Understanding the Roles of Excipients in Moisture Management in Solid Dosage Forms
    Veronica N, Heng PWS, Liew CV
    Mol Pharm, 2024 May 06;21(5):2484-2500.
    PMID: 38647432 DOI: 10.1021/acs.molpharmaceut.4c00031
    Excipients are ubiquitous in pharmaceutical products, and often, they can also play a critical role in maintaining product quality. For a product containing a moisture-sensitive drug, moisture can be deleterious to the product stability during storage. Therefore, using excipients that interact with moisture in situ can potentially alleviate product stability issues. In this study, the interactive behavior of starch with moisture was augmented by coprocessing maize starch with sodium chloride (NaCl) or magnesium nitrate hexahydrate [Mg(NO3)2·6H2O] at different concentrations (5 and 10%, w/w). The effect of the formulation on drug stability was assessed through the degradation of acetylsalicylic acid, which was used as the model drug. The results showed that coprocessing of the starch with either NaCl or Mg(NO3)2·6H2O impacted the number of water molecule binding sites on the starch and how the sorbed moisture was distributed. The coprocessed excipients also resulted in lower drug degradation and lesser changes in tablet tensile strength during post-compaction storage. However, corresponding tablet formulations containing physical mixtures of starch and salts did not yield promising outcomes. This study demonstrated the advantageous concomitant use of common excipients by coprocessing to synergistically mitigate the adverse effects of moisture and promote product stability when formulating a moisture-sensitive drug. In addition, the findings could help to improve the understanding of moisture-excipient interactions and allow for the judicious choice of excipients when designing formulations containing moisture-sensitive drugs.
    Matched MeSH terms: Drug Compounding/methods
  12. Thermal sintering: a novel technique used in the design, optimization and biopharmaceutical evaluation of propranolol HCl gastric floating tablets
    Venkata Srikanth M, Songa AS, Nali SR, Battu JR, Kolapalli VR
    Drug Dev Ind Pharm, 2014 Jan;40(1):33-45.
    PMID: 23317339 DOI: 10.3109/03639045.2012.744416
    The objective of the present investigation was to study the applicability of thermal sintering technique for the development of gastric floating tablets of propranolol HCl. Formulations were prepared using four independent variables, namely (i) polymer quantity, (ii) sodium bicarbonate concentration, (iii) sintering temperature and (iv) sintering time. Floating lag time and t95 were taken as dependent variables. Tablets were prepared by the direct compression method and were evaluated for physicochemical properties, in vitro buoyancy and dissolution studies. From the drug release studies, it was observed that drug retarding property mainly depends upon the sintering temperature and time of exposure. The statistically optimized formulation (PTSso) was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry studies, and no significant chemical interaction between drug and polymer was observed. Optimized formulation was stable at accelerated conditions for a period of six months. PTSso was evaluated for in vivo buoyancy studies in humans for both fed and fasted states and found that gastric residence time of the floating tablets were enhanced by fed stage but not in fasted state. Optimized formulation PTSso and commercial formulation Ciplar LA 80 were subjected to bioavailability studies in healthy human volunteers by estimating pharmacokinetic parameters such as Cmax, Tmax, area under curve (AUC), elimination rate constant (Kel), biological half-life (t1/2) and mean residence time (MRT). There was a significant increase in the bioavailability of the propranolol HCl from PTSso formulation, which was evident from increased AUC levels and larger MRT values than Ciplar LA 80.
    Matched MeSH terms: Drug Compounding/methods
  13. Fulltext Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum)
    Meka VS, Nali SR, Songa AS, Kolapalli VR
    AAPS PharmSciTech, 2012 Dec;13(4):1451-64.
    PMID: 23090110 DOI: 10.1208/s12249-012-9873-5
    The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosage form is exposed to gastrointestinal fluids in the gastric environment. As BG was being explored for the first time for its pharmaceutical application, physicochemical, microbiological, rheological, and stability studies were carried out on this gum. In the present investigation, the physicochemical properties, such as micromeritic, rheological, melting point, moisture content, pH, swelling index, water absorption, and volatile acidity, were evaluated. The gum was characterized by scanning electron microscopy, differential scanning calorimetry (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR). Gastroretentive floating tablets of BG were prepared with the model drug propranolol HCl by direct compression methods. The prepared tablets were evaluated for all their physicochemical properties, in vitro buoyancy, in vitro drug release, and rate order kinetics. PBG 04 was selected as an optimized formulation based on its 12-h drug release and good buoyancy characteristics. The optimized formulation was characterized with FTIR, DSC, and PXRD studies, and no interaction between the drug and BG was found. Thus, the study confirmed that BG might be used in the gastroretentive drug delivery system as a release-retarding polymer.
    Matched MeSH terms: Drug Compounding/methods
  14. The use of dimethyl sulfoxide in contact lens disinfectants is a potential preventative strategy against contracting Acanthamoeba keratitis
    Siddiqui R, Aqeel Y, Khan NA
    Cont Lens Anterior Eye, 2016 Oct;39(5):389-93.
    PMID: 27133448 DOI: 10.1016/j.clae.2016.04.004
    Acanthamoeba castellanii is the causative agent of blinding keratitis. Though reported in non-contact lens wearers, it is most frequently associated with improper use of contact lens. For contact lens wearers, amoebae attachment to the lens is a critical first step, followed by amoebae binding to the corneal epithelial cells during extended lens wear. Acanthamoeba attachment to surfaces (biological or inert) and migration is an active process and occurs during the trophozoite stage. Thus retaining amoebae in the cyst stage (dormant form) offers an added preventative measure in impeding parasite traversal from the contact lens onto the cornea. Here, we showed that as low as 3% DMSO, abolished A. castellanii excystation. Based on the findings, it is proposed that DMSO should be included in the contact lens disinfectants as an added preventative strategy against contracting Acanthamoeba keratitis.
    Matched MeSH terms: Drug Compounding/methods
  15. Fulltext Formulation and delivery of itraconazole to the brain using a nanolipid carrier system
    Lim WM, Rajinikanth PS, Mallikarjun C, Kang YB
    Int J Nanomedicine, 2014;9:2117-26.
    PMID: 24833900 DOI: 10.2147/IJN.S57565
    The objectives of this study were to develop and characterize itraconazole (ITZ)-loaded nanostructured lipid carriers (NLCs) and to study their potential for drug delivery into the brain. Precirol(®) ATO 5 and Transcutol(®) HP were selected as the lipid phase, and Tween(®) 80 and Solutol(®) HS15 as surfactants. The ITZ-NLCs were prepared by a hot and high-pressure homogenization method. The entrapment efficiency for the best formulation batch was analyzed using high-performance liquid chromatography and was found to be 70.5%±0.6%. The average size, zeta potential, and polydispersity index for the ITZ-NLCs used for animal studies were found to be 313.7±15.3 nm, -18.7±0.30 mV, and 0.562±0.070, respectively. Transmission electron microscopy confirmed that ITZ-NLCs were spherical in shape, with a size of less than 200 nm. Differential scanning calorimetry and X-ray diffractometry analysis showed that ITZ was encapsulated in the lipid matrix and present in the amorphous form. The in vitro release study showed that ITZ-NLCs achieved a sustained release, with cumulative release of 80.6%±5.3% up to 24 hours. An in vivo study showed that ITZ-NLCs could increase the ITZ concentration in the brain by almost twofold. These results suggest that ITZ-NLCs can be exploited as nanocarriers to achieve sustained release and brain-targeted delivery.
    Matched MeSH terms: Drug Compounding/methods
  16. Encapsulation of caffeine into starch matrices: Bitterness evaluation and suppression mechanism
    Shao M, Li S, Tan CP, Kraithong S, Gao Q, Fu X, et al.
    Int J Biol Macromol, 2021 Mar 15;173:118-127.
    PMID: 33444656 DOI: 10.1016/j.ijbiomac.2021.01.043
    In this study, caffeine (CA) was encapsulated into food-grade starch matrices, including swelled starch (SS), porous starch (PS), and V-type starch (VS). The bitterness of the microcapsules and suppression mechanisms were investigated using an electronic tongue, molecular dynamics (MD) simulation and the in vitro release kinetics of CA. All the CA-loaded microcapsules showed a lower bitterness intensity than the control. The MD results proved that the weak interactions between starch and CA resulted in a moderate CA release rate for SS-CA microcapsules. The PS-CA microcapsule presented the longest CA release, up to 40 min, whereas the VS-CA microcapsule completely released CA in 9 min. The CA release rate was found to be related to the microcapsule structure and rehydration properties. A low CA bitterness intensity could be attributed to a delay in the CA release rate and resistance to erosion of the microcapsules. The results of this work are valuable for improving starch-based microcapsules (oral-targeted drug-delivery systems) by suppressing the bitterness of alkaloid compounds.
    Matched MeSH terms: Drug Compounding/methods*
  17. Fulltext Microencapsulation of Lactococcus lactis Gh1 with Gum Arabic and Synsepalum dulcificum via Spray Drying for Potential Inclusion in Functional Yogurt
    Fazilah NF, Hamidon NH, Ariff AB, Khayat ME, Wasoh H, Halim M
    Molecules, 2019 Apr 11;24(7).
    PMID: 30978923 DOI: 10.3390/molecules24071422
    There has been an explosion of probiotic incorporated based product. However, many reports indicated that most of the probiotics have failed to survive in high quantity, which has limited their effectiveness in most functional foods. Thus, to overcome this problem, microencapsulation is considered to be a promising process. In this study, Lactococcus lactis Gh1 was encapsulated via spray-drying with gum Arabic together with Synsepalum dulcificum or commonly known as miracle fruit. It was observed that after spray-drying, high viability (~10⁸ CFU/mL) powders containing L. lactis in combination with S. dulcificum were developed, which was then formulated into yogurt. The tolerance of encapsulated bacterial cells in simulated gastric juice at pH 1.5 was tested in an in-vitro model and the result showed that after 2 h, cell viability remained high at 1.11 × 10⁶ CFU/mL. Incubation of encapsulated cells in the presence of 0.6% (w/v) bile salts showed it was able to survive (~10⁴ CFU/mL) after 2 h. Microencapsulated L. lactis retained a higher viability, at ~10⁷ CFU/mL, when incorporated into yogurt compared to non-microencapsulated cells ~10⁵ CFU/mL. The fortification of microencapsulated and non-microencapsulated L. lactis in yogurts influenced the viable cell counts of yogurt starter cultures, Lactobacillus delbrueckii subs. bulgaricus and Streptococcus thermophilus.
    Matched MeSH terms: Drug Compounding/methods
  18. Ionic-Liquid-Based Paclitaxel Preparation: A New Potential Formulation for Cancer Treatment
    Chowdhury MR, Moshikur RM, Wakabayashi R, Tahara Y, Kamiya N, Moniruzzaman M, et al.
    Mol Pharm, 2018 06 04;15(6):2484-2488.
    PMID: 29762034 DOI: 10.1021/acs.molpharmaceut.8b00305
    Paclitaxel (PTX) injection (i.e., Taxol) has been used as an effective chemotherapeutic treatment for various cancers. However, the current Taxol formulation contains Cremophor EL, which causes hypersensitivity reactions during intravenous administration and precipitation by aqueous dilution. This communication reports the preliminary results on the ionic liquid (IL)-based PTX formulations developed to address the aforementioned issues. The formulations were composed of PTX/cholinium amino acid ILs/ethanol/Tween-80/water. A significant enhancement in the solubility of PTX was observed with considerable correlation with the density and viscosity of the ILs, and with the side chain of the amino acids used as anions in the ILs. Moreover, the formulations were stable for up to 3 months. The driving force for the stability of the formulation was hypothesized to be the involvement of different types of interactions between the IL and PTX. In vitro cytotoxicity and antitumor activity of the IL-based formulations were evaluated on HeLa cells. The IL vehicles without PTX were found to be less cytotoxic than Taxol, while both the IL-based PTX formulation and Taxol exhibited similar antitumor activity. Finally, in vitro hypersensitivity reactions were evaluated on THP-1 cells and found to be significantly lower with the IL-based formulation than Taxol. This study demonstrated that specially designed ILs could provide a potentially safer alternative to Cremophor EL as an effective PTX formulation for cancer treatment giving fewer hypersensitivity reactions.
    Matched MeSH terms: Drug Compounding/methods
  19. Preparation, characterization, and in vivo evaluation of insulin-loaded PLA-PEG microspheres for controlled parenteral drug delivery
    Sheshala R, Peh KK, Darwis Y
    Drug Dev Ind Pharm, 2009 Nov;35(11):1364-74.
    PMID: 19832637 DOI: 10.3109/03639040902939213
    AIM: The aim of this study was to prepare insulin-loaded poly(lactic acid)-polyethylene glycol microspheres that could control insulin release at least for 1 week and evaluate their in vivo performance in a streptozotocin-induced diabetic rat model.
    METHODS: The microspheres were prepared using a water-in-oil-in-water double emulsion solvent evaporation technique. Different formulation variables influencing the yield, particle size, entrapment efficiency, and in vitro release profiles were investigated. The pharmacokinetic study of optimized formulation was performed with single dose in comparison with multiple dose of Humulin 30/70 as a reference product in streptozotocin-induced diabetic rats.
    RESULTS: The optimized formulation of insulin microspheres was nonporous, smooth-surfaced, and spherical in structure under scanning electron microscope with a mean particle size of 3.07 microm and entrapment efficiency of 42.74% of the theoretical amount incorporated. The in vitro insulin release profiles was characterized by a bimodal behavior with an initial burst release because of the insulin adsorbed on the microsphere surface, followed by slower and continuous release corresponding to the insulin entrapped in polymer matrix.
    CONCLUSIONS: The optimized formulation and reference were comparable in the extent of absorption. Consequently, these microspheres can be proposed as new controlled parenteral delivery system.
    Matched MeSH terms: Drug Compounding/methods*
  20. Technical aspects of preparing PEG-PLGA nanoparticles as carrier for chemotherapeutic ‎agents by nanoprecipitation method
    Almoustafa HA, Alshawsh MA, Chik Z
    Int J Pharm, 2017 Nov 25;533(1):275-284.
    PMID: 28943210 DOI: 10.1016/j.ijpharm.2017.09.054
    Nanoprecipitation is a simple and increasingly trending method for nanoparticles preparation. The self-assembly feature of poly (ethylene glycol)-poly (lactide-co-glycolic acid) (PEG-PLGA) amphiphilic copolymer into a nanoparticle and its versatile structure makes nanoprecipitation one of the best methods for its preparation. The aim of this study is to review currently available literature for standard preparation of PEG-PLGA nanoparticles using nanoprecipitation technique in order to draw conclusive evidenceto draw conclusive evidence that can guide researchers during formulation development. To achieve this, three databases (Web of Science, Scopus and PubMed) were searched using relevant keywords and the extracted articles were reviewed based on defined inclusion and exclusion criteria. Data extraction and narrative analysis of the obtained literature was performed when appropriate, along with our laboratory observations to support those claims wherever necessary. As a result of this analysis, reports that matched our criteria conformed to the general facts about nanoprecipitation techniques such as simplicity in procedure, low surfactants requirement, narrow size distribution, and low resulting concentrations. However, these reports showed interesting advantages for using PEG-PLGA as they are frequently reported to be freeze-dried and active pharmaceutical ingredients (APIs) with low hydrophobicity were reported to successfully be encapsulated in the particles.
    Matched MeSH terms: Drug Compounding/methods*
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