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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
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*
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
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
Fulltext Preparation of Fe₃O₄ magnetic nanoparticles coated with gallic acid for drug delivery

Dorniani D, Hussein MZ, Kura AU, Fakurazi S, Shaari AH, Ahmad Z

Int J Nanomedicine, 2012;7:5745-56.
PMID: 23166439 DOI: 10.2147/IJN.S35746

Magnetic iron oxide nanoparticles were prepared using a sonochemical method under atmospheric conditions at a Fe²⁺ to Fe³⁺ molar ratio of 1:2. The iron oxide nanoparticles were subsequently coated with chitosan and gallic acid to produce a core-shell structure.

Matched MeSH terms: Drug Compounding/methods
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
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
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*
Effects of Accelerated Storage on the Quality of Kenaf Seed Oil in Chitosan-Coated High Methoxyl Pectin-Alginate Microcapsules

Leong MH, Tan CP, Nyam KL

J Food Sci, 2016 Oct;81(10):C2367-C2372.
PMID: 27635525 DOI: 10.1111/1750-3841.13442

The objective of this research was to study the oxidative stability and antioxidant properties of microencapsulated kenaf (Hibiscus cannabinus L.) seed oil (MKSO) produced by co-extrusion technology upon accelerated storage. The combination of sodium alginate, high methoxyl pectin, and chitosan were used as shell materials. The oxidative stability of the kenaf seed oil was determined by iodine value, peroxide value, p-Anisidine value, total oxidation (TOTOX), thiobarbituric acid reactive substances assay, and free fatty acid content. Total phenolic content, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) cation radical-scavenging assay and 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay were used to examine the antioxidant properties of oils. Oxidative stability tests showed that bulk kenaf seed oil (BKSO) was oxidized significantly higher (P < 0.05) than MKSO. The total increment of TOTOX value of BKSO was 165.93% significantly higher (P < 0.05) than MKSO. Co-extrusion technology has shown to be able to protect kenaf seed oil against lipid oxidation and delay the degradation of natural antioxidants that present in oil during storage.

Matched MeSH terms: Drug Compounding*
Effect of Gum Arabic, β-Cyclodextrin, and Sodium Caseinate as Encapsulating Agent on the Oxidative Stability and Bioactive Compounds of Spray-Dried Kenaf Seed Oil

Chew SC, Tan CP, Nyam KL

J Food Sci, 2018 Sep;83(9):2288-2294.
PMID: 30074623 DOI: 10.1111/1750-3841.14291

Kenaf seed oil is prone to undergo oxidation due to its high content of unsaturated fatty acids, thus microencapsulation stands as an alternative to protect kenaf seed oil from the adverse environment. This study primarily aimed to evaluate the oxidative stability of microencapsulated refined kenaf seed oil (MRKSO) by the use of gum arabic, β-cyclodextrin, and sodium caseinate as the wall materials by spray drying. Bulk refined kenaf seed oil (BRKSO) and MRKSO were kept at 65 °C for 24 days to evaluate its oxidative stability, changes of tocopherol and tocotrienol contents, phytosterol content, and fatty acid profile. The results showed that the peroxide value, p-Anisidine value, and total oxidation value of BRKSO were significantly higher than the MRKSO at day 24. The total tocopherol and tocotrienol contents were reduced 66.1% and 56.8% in BRKSO and MRKSO, respectively, upon the storage. There was a reduction of 71.7% and 23.5% of phytosterol content in BRKSO and MRKSO, respectively, upon the storage. The degradation rate of polyunsaturated fatty acids in BRKSO was higher than that of MRKSO. This study showed that the current microencapsulation technique is a feasible way to retard the oxidation of kenaf seed oil.
PRACTICAL APPLICATION: There is increasing research on the functional properties of crude kenaf seed oil, but the crude kenaf seed oil is not edible. This study offered in developing of microencapsulated refined kenaf seed oil by spray drying, which is suitable for food application. The microencapsulation of refined kenaf seed oil with healthier wall materials is beneficial in developing a diversity of functional food products and supplements.

Matched MeSH terms: Drug Compounding/methods*
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
Investigation on the effect of polymer and starch on the tablet properties of lyophilized orally disintegrating tablet

Liew KB, Peh KK

Arch Pharm Res, 2021 Aug;44(8):1-10.
PMID: 25579848 DOI: 10.1007/s12272-014-0542-y

Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.

Matched MeSH terms: Drug Compounding/methods
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
Vesicular Systems Containing Curcumin and Their Applications in Respiratory Disorders - A Mini Review

Chellappan DK, Hansbro PM, Dua K, Hsu A, Gupta G, Ng ZY, et al.

Pharm Nanotechnol, 2017;5(4):250-254.
PMID: 28786351 DOI: 10.2174/2211738505666170808094635

BACKGROUND: Vesicular systems like nanotechnology and liposomes are gaining tremendous attention lately in the field of respiratory diseases. These formulations enhance bioavailability of the drug candidate, which could be achieved through a novel drug delivery mechanism. Moreover, the therapeutic potential achieved through these systems is highly controllable over long durations of time providing better efficacy and patient compliance.
OBJECTIVE: The objective of this paper is to review the recent literature on vesicular drug delivery systems containing curcumin.
METHODS: We have collated and summarized various recent attempts made to develop different controlled release drug delivery systems containing curcumin which would be of great interest for herbal, formulation and biological scientists. There are several vesicular nanotechnological techniques involving curcumin which have been studied recently, targeting pulmonary diseases.
RESULTS: Different vesicular systems containing curcumin are being studied for their therapeutic potential in different respiratory diseases. There has been a renewed interest in formulations containing curcumin recently, primarily owing to the broad spectrum therapeutic potential of this miracle substance. Various types of formulations, containing curcumin, targeting different bodily systems have recently emerged and, nevertheless, the search for newer frontiers with this drug goes on.
CONCLUSION: This mini review, in this direction, tries to highlight the key research interventions employing vesicular systems of drug delivery with curcumin.

Matched MeSH terms: Drug Compounding/methods
Fulltext Nano-Formulation of Ethambutol with Multifunctional Graphene Oxide and Magnetic Nanoparticles Retains Its Anti-Tubercular Activity with Prospects of Improving Chemotherapeutic Efficacy

Saifullah B, Maitra A, Chrzastek A, Naeemullah B, Fakurazi S, Bhakta S, et al.

Molecules, 2017 Oct 12;22(10).
PMID: 29023384 DOI: 10.3390/molecules22101697

Tuberculosis (TB) is a dreadful bacterial disease, infecting millions of human and cattle every year worldwide. More than 50 years after its discovery, ethambutol continues to be an effective part of the World Health Organization's recommended frontline chemotherapy against TB. However, the lengthy treatment regimens consisting of a cocktail of antibiotics affect patient compliance. There is an urgent need to improve the current therapy so as to reduce treatment duration and dosing frequency. In this study, we have designed a novel anti-TB multifunctional formulation by fabricating graphene oxide with iron oxide magnetite nanoparticles serving as a nano-carrier on to which ethambutol was successfully loaded. The designed nanoformulation was characterised using various analytical techniques. The release of ethambutol from anti-TB multifunctional nanoparticles formulation was found to be sustained over a significantly longer period of time in phosphate buffer saline solution at two physiological pH (7.4 and 4.8). Furthermore, the nano-formulation showed potent anti-tubercular activity while remaining non-toxic to the eukaryotic cells tested. The results of this in vitro evaluation of the newly designed nano-formulation endorse its further development in vivo.

Matched MeSH terms: Drug Compounding*
Fulltext Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide

Saifullah B, Chrzastek A, Maitra A, Naeemullah B, Fakurazi S, Bhakta S, et al.

Molecules, 2017 Oct 12;22(10).
PMID: 29023399 DOI: 10.3390/molecules22101560

Tuberculosis (TB) is a bacterial disease responsible for millions of infections and preventable deaths each year. Its treatment is complicated by patients' noncompliance due to dosing frequency, lengthy treatment, and adverse side effects associated with current chemotherapy. However, no modifications to the half-a-century old standard chemotherapy have been made based on a nanoformulation strategy to improve pharmacokinetic efficacy. In this study, we have designed a new nanodelivery formulation, using graphene oxide as the nanocarrier, loaded with the anti-TB antibiotic, ethambutol. The designed formulation was characterized using a number of molecular analytical techniques. It was found that sustained release of the drug resulted in better bioavailability. In addition, the designed formulation demonstrated high biocompatibility with mouse fibroblast cells. The anti-TB activity of the nanodelivery formulation was determined using whole-cell resazurin microtiter plate assay, modified-spot culture growth inhibition assay, and biofilm inhibition assay. The nanodelivery formulation showed good anti-mycobacterial activity. The anti-mycobacterial activity of Ethambutol was unaffected by the drug loading and release process. The results of this study demonstrated the potential of this new nanodelivery formulation strategy to be considered for modifying existing chemotherapy to yield more efficacious antibiotic treatment against TB.

Matched MeSH terms: Drug Compounding*
Fulltext Eco-friendly synthesis of silver nanoparticles and its larvicidal property against fourth instar larvae of Aedes aegypti

Ali ZA, Roslan MA, Yahya R, Wan Sulaiman WY, Puteh R

IET Nanobiotechnol, 2017 Mar;11(2):152-156.
PMID: 28476997 DOI: 10.1049/iet-nbt.2015.0123

In this study, larvicidal activity of silver nanoparticles (AgNPs) synthesised using apple extract against fourth instar larvae of Aedes aegypti was determined. As a result, the AgNPs showed moderate larvicidal effects against Ae. aegypti larvae (LC50 = 15.76 ppm and LC90 = 27.7 ppm). In addition, comparison of larvicidal activity performance of AgNPs at high concentration prepared using two different methods showed that Ae. aegypti larvae was fully eliminated within the duration of 2.5 h. From X-ray diffraction, the AgNP crystallites were found to exhibit face centred cubic structure. The average size of these AgNPs as estimated by particle size distribution was in the range of 50-120 nm. The absorption maxima of the synthesised Ag showed characteristic Ag surface plasmon resonance peak. This green synthesis provides an economic, eco-friendly and clean synthesis route to Ag.

Matched MeSH terms: Drug Compounding/methods
Fulltext Empty nano and micro-structured lipid carriers of virgin coconut oil for skin moisturisation

Noor NM, Khan AA, Hasham R, Talib A, Sarmidi MR, Aziz R, et al.

IET Nanobiotechnol, 2016 Aug;10(4):195-9.
PMID: 27463789 DOI: 10.1049/iet-nbt.2015.0041

Virgin coconut oil (VCO) is the finest grade of coconut oil, rich in phenolic content, antioxidant activity and contains medium chain triglycerides (MCTs). In this work formulation, characterisation and penetration of VCO-solid lipid particles (VCO-SLP) have been studied. VCO-SLP were prepared using ultrasonication of molten stearic acid and VCO in an aqueous solution. The electron microscopy imaging revealed that VCO-SLP were solid and spherical in shape. Ultrasonication was performed at several power intensities which resulted in particle sizes of VCO-SLP ranged from 0.608 ± 0.002 µm to 44.265 ± 1.870 µm. The particle size was directly proportional to the applied power intensity of ultrasonication. The zeta potential values of the particles were from -43.2 ± 0.28 mV to -47.5 ± 0.42 mV showing good stability. The cumulative permeation for the smallest sized VCO-SLP (0.608 µm) was 3.83 ± 0.01 µg/cm(2) whereas for larger carriers it was reduced (3.59 ± 0.02 µg/cm(2)). It is concluded that SLP have the potential to be exploited as a micro/nano scale cosmeceutical carrying vehicle for improved dermal delivery of VCO.

Matched MeSH terms: Drug Compounding/methods
Fulltext Exploring the potential of a highly compressible microcrystalline cellulose as novel tabletting excipient in the compaction of extended-release coated pellets containing an extremely water-soluble model drug

Zeeshan F, Peh KK, Tan YT

AAPS PharmSciTech, 2009;10(3):850-7.
PMID: 19554454 DOI: 10.1208/s12249-009-9278-2

Compaction of controlled-release coated pellets into tablets is challenging because of the fusion of pellets and the rupturing of coated film. The difficulty in compaction intensifies with the use of extremely water-soluble drugs. Therefore, the present study was conducted to prepare and compact pellets containing pseudoephedrine hydrochloride as an extremely water-soluble model drug. The pellets were produced using an extrusion-spheronization technique. The drug-loaded pellets were coated to extend the drug release up to 12-h employing various polymers, and then they were compressed into tablets using microcrystalline cellulose Ceolus KG-801 as a novel tabletting excipient. The in vitro drug release studies of coated pellets and tablets were undertaken using the USP basket method in dissolution test apparatus I. The amount of drug released was analyzed at a wavelength of 215 nm. The combined coatings of hydroxypropyl methylcellulose and Kollicoat SR-30D yielded 12-h extended-release pellets with drug release independent of pH of dissolution medium following zero-order kinetics. The drug release from the tablets prepared using inert Celous KG-801 granules as tabletting excipient was found faster than that of coated pellets. However, a modification in drug release rate occurred with the incorporation of inert Ceolus KG-801 pellets. The drug dissolution profile from tablets containing 40% w/w each of coated pellets and inert granules along with 20% w/w inert pellets was found to be closely similar to that of coated pellets. Furthermore, the friability, tensile strength, and disintegration time of the tablets were within the USP specifications.

Matched MeSH terms: Drug Compounding
In vitro controlled release of alfuzosin hydrochloride using HPMC-based matrix tablets and its comparison with marketed product

Nair A, Gupta R, Vasanti S

Pharm Dev Technol, 2007;12(6):621-5.
PMID: 18161635

The present study is an attempt to formulate a controlled-release matrix tablet formulation for alfuzosin hydrochloride by using low viscous hydroxy propyl methyl cellulose (HPMC K-100 and HPMC 15cps) and its comparison with marketed product. Different batches of tablets containing 10 mg of alfuzosin were prepared by direct compression technique and evaluated for their physical properties, drug content, and in vitro drug release. All the formulations had a good physical integrity, and the drug content between the batches did not vary by more than 1%. Drug release from the matrix tablets was carried out for 12 hr and showed that the release rate was not highly significant with different ratios of HPMC K-100 and HPMC15cps. Similar dissolution profiles were observed between formulation F3 and the marketed product throughout the study period. The calculated regression coefficients showed a higher r2 value with zero-order kinetics and Higuchi model in all the cases. Although both the models could be applicable, zero-order kinetics seems to be better. Hence, it can be concluded that the use of low viscous hydrophilic polymer of different grades (HPMC K-100 and HPMC 15cps) can control the alfuzosin release for a period of 12 hr and was comparable to the marketed product.

Matched MeSH terms: Drug Compounding

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