A W/O emulsion mediated film dispersion method for curcumin encapsulated pH-sensitive liposomes in the colon tumor treatment.
Authors: Chen Y, Du Q, Guo Q, Huang J, Liu L, Shen X, Peng J Abstract The CaCO3 encapsulated liposome with pH sensitivity is an efficient carrier for the delivery of chemotherapeutic drugs. Herein, we provided an innovative method that take advantage of a W/O emulsion to prepare CaCO3 encapsulated liposomes for the delivery of curcumin. The liposomes with both CaCO3 and curcumin encapsulated (LCC) showed highly sensitivity to reduced pH (the environment of lysosomes). Due to the inherent pH sensitivity of CaCO3, LCC swelled and released the encapsulated curcumin rapidly in acidic medium. The lysosome escape capabil...
Source: Drug Development and Industrial Pharmacy - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development and evaluation of hollow mesoporous silica microspheres bearing on enhanced oral delivery of curcumin.
In conclusion, this system demonstrated a great potential for efficiently delivery of curcumin in vitro and in vivo, suggesting a good prospect for its application in clinic for therapeutic drug delivery in future. PMID: 30346852 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

The effect of ferrous ions, calcium ions and citric acid on absorption of ciprofloxacin across caco-2 cells: practical and structural approach.
CONCLUSIONS: The size of the formed complexes, rather than the decrease in the solubility of formed complexes, plays a significant role in permeation (absorption) of Cipro. CitA might ameliorate the effect of co-administered metal ions on the bioavailability of Cipro. PMID: 30348012 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Formulation-optimization of solid lipid nanocarrier system of STAT3 inhibitor to improve its activity in triple negative breast cancer cells.
In conclusion, the results of the present study demonstrate that the formulation of Niclo as SLNs will improve the anticancer efficacy against TNBC. PMID: 30348020 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Microneedles for Transdermal Drug Delivery: A Systematic Review.
Authors: Dharadhar S, Majumdar A, Dhoble S, Patravale V Abstract Transdermal route has been explored for various agents due to its advantage of by passing the first pass effect and sustained release of drug. Due to strong barrier properties of the skin, mainly stratum corneum (SC), the delivery of many therapeutic agents across the skin has become challenging. Few drugs with specific physicochemical properties (molecular weight
Source: Drug Development and Industrial Pharmacy - October 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Tolmetin Sodium loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks.
Authors: Akl MA, Ismael HR, Abd Allah FI, Kassem AA, Samy AM Abstract Tolmetin sodium (TS) is a non-steroidal anti-inflammatory drug (NSAID) indicated for treatment of musculoskeletal issues. As other NSAID, TS displays a marked side effects on the gastro-intestinal (GI) tract after oral administration. Tradational solid suppositories can cause pain and discomfort for patients, may reach the end of the colon; consequently, the drug can undergo the first-pass effect. TS liquid suppository (TS-LS) was developed to enhance patient compliance and rectal mucosal safety in high-risk patients receiving highly NSAID therap...
Source: Drug Development and Industrial Pharmacy - October 13, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Simultaneous Determination of Methocarbamol and Aspirin in Presence of their Pharmacopeial Related Substances in Combined.
CONCLUSION: The optimized method proved to be specific, robust and precise for the quality control of the studied drugs in pharmaceutical preparations to ascertain that their related substances are not exceeding the permitted pharmacopeial limits. PMID: 30307339 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - October 13, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Vitamin B12 buccoadhesive tablets; auspicious non-invasive substitute for intra muscular injection: Formulation, In-vitro and In-vivo appraisal.
Authors: Ali SM, Abdelkader H, Elrehany M, Fathi Mansour H Abstract Attempting to prepare a convenient bioavailable formulation of vitamin B12 (cyanocobalamin), seventeen tablet formulations were prepared by direct compression. Different concentrations of hydroxypropyl methyl cellulose (HPMC), carbopol 971p (CP971p) and chitosan (Cs) were used. The tablets were characterized for thickness, weight, drug content, hardness, friability, surface pH, in-vitro drug release and mucoadhesion. Kinetic analysis of the release data was conducted. Vitamin B12 bioavailability from the optimized formulations was studied on rabbit...
Source: Drug Development and Industrial Pharmacy - October 7, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Oil-entrapped Ranitidine HCl Beads Heal Peptic Ulcers Via Local and Systemic Mechanisms.
CONCLUSIONS: floating oil-entrapped beads are a promising approach for RHCl delivery to remain in stomach for a longer time ensuring site-specific delivery and consequently, enhancing local healing effect of peptic ulcers. PMID: 30260710 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 29, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Smart systems for determination of drug's solubility.
Authors: Jouyban-Gharamaleki V, Jouyban A, Acree WE, Rahimpour E Abstract The solubility of drugs is a crucial physicochemical property in the drug discovery or development process and for improving the bioavailability of drugs. There are various methods for evaluating the solubility of drugs including manual measurement methods, mathematical methods and smart methods. Manual measurement and mathematical methods have some defects which make the smart systems more reliable and important in this field. In this review, various instruments used for the solubility determination, along with the smart systems, have been d...
Source: Drug Development and Industrial Pharmacy - September 29, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Stability investigation of FCC-based tablets for oral suspension with caffeine and oxantel pamoate as model drugs.
In this study, the influence of formulation composition on disintegration time in water and artificial saliva was investigated using caffeine and oxantel pamoate as model drugs, reflecting BCS class 1 and BCS class 4, respectively. The optimized formulation for each model drug underwent a stress test. The results show that the drug content in DTs was not influenced by FCC under stressed conditions, however the disintegration and dissolution performance was affected by temperature and humidity. It can be concluded that it was possible to produce TOS characterized by rapid disintegration complemented by high physical stabili...
Source: Drug Development and Industrial Pharmacy - September 29, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Complexation of novel thiomers and insulin to protect against in vitro enzymatic degradation - towards oral insulin delivery.
Authors: Ibie CO, Knott RM, Thompson CJ Abstract A significant barrier to oral insulin delivery is its enzymatic degradation in the gut. Nano-sized polymer-insulin polyelectrolyte complexes (PECS) have been developed to protect insulin against enzymatic degradation. Poly(allylamine) (Paa) was trimethylated to yield QPaa. Thiolation of Paa and QPaa was achieved by attaching either N-acetylcysteine (NAC) or thiobutylamidine (TBA) ligands (Paa-NAC/QPaa-NAC and Paa-TBA/QPaa-TBA thiomers). PEC formulations were prepared in Tris buffer (pH 7.4) at various polymer: insulin mass ratios (0.2:1-2:1). PECS were characterized ...
Source: Drug Development and Industrial Pharmacy - September 27, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

1,3-dimethyl-6-nitroacridine derivatives induce apoptosis in human breast cancer cells by targeting DNA.
Authors: Zhou Q, Wu H, You C, Gao Z, Sun K, Wang M, Chen F, Sun B Abstract The acridine derivatives can interact with the double stranded DNA, which is regarded as the biological target of the anticancer drugs in cancer treatment. We designed, and synthesized a new series of 1,3-dimethyl-6-nitroacridine derivatives as potential DNA-targeted anticancer agents. These compounds could partially intercalate into the calf thymus DNA, differing from the parent acridine. The results showed that the substitutions of the acridine ring had great effect on DNA binding affinity. The binding constants determined by UV-vis spectr...
Source: Drug Development and Industrial Pharmacy - September 27, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

A case study where pharmaceutical salts were used to address the issue of low in vivo exposure.
In conclusion, this study showed that three salts of a new selected candidate drug could be used to improve solubility, increase dissolution rate and enhance oral absorption compared with a more commonly used nanocrystal formulation of the API. However, the identity of the counter ion appeared to be of less importance. On the other hand, only the salt of the hemi-1.5-naphtalenedisulphonic acid seemed to improve chemical stability compared with the API. PMID: 30256689 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 27, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Mechanism of enhanced oral absorption of Akebia saponin D by a self-nanoemulsifying drug delivery system loaded with phospholipid complex.
Authors: Wang Y, Shen J, Yang X, Jin Y, Yang Z, Wang R, Zhang F, Linhardt RJ Abstract Akebia saponin D (ASD) exhibits a variety of pharmacological activities, such as anti-osteoporosis, neuroprotection, hepatoprotection, but has poor oral bioavailability. A self-nanoemulsifying drug delivery system loaded with akebia saponin D - phospholipid complex (APC-SNEDDS) (composition: Peceol: Cremophor® EL: Transcutol HP: ASD: phospholipid; ratio: 10:45:45:51:12.3, w:w:w:w:w) was first developed to improve the oral absorption of saponins and it was found to significantly enhance ASD's oral bioavailability by 4.3 - fold (P
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Brain targeting of chitosan-based diazepam mucoadhesive micro emulsions via nasal route: Formulation optimization, characterization, Pharmacokinetic and Pharmacodynamic evaluations.
Authors: Ramreddy S, Janapareddi K Abstract OBJECTIVE: The aim of present investigation was to develop Micro Emulsions (ME) and Mucoadhesive Micro Emulsions (MME) of Diazepam for brain uptake through nasal administration for the treatment of seizure emergency. SIGNIFICANCE: Status Epilepticus (SE) is a medical emergency, requires intravenous administration of diazepam which requires hospitalization of patient. Initiation of therapy at home via nasal administration of diazepam could prevent the damage of brain due to delay of therapy initiation. METHODS: Diazepam MEs were prepared by phase titration method, ...
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Dissolution or Disintegration - Substitution of Dissolution by Disintegration Testing for a Fixed Dose Combination Product.
Authors: Grube A, Gerlitzki C, Brendel M Abstract According to ICH guideline Q6A, dissolution testing can be replaced by disintegration testing if it can be shown that the active pharmaceutical ingredient (API) is highly soluble and the formulation is rapidly releasing. In addition, a relationship between dissolution and disintegration has to be established. For a fixed-dose combination tablet of empagliflozin and linagliptin this relationship was established by applying two different approaches. In the first approach, the extent to which the disintegration process of the film-coated tablets contributes to the rele...
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

SCC4 cell monolayers as an alternative sublingual barrier model: influence of nanoencapsulation on carvedilol transport.
CONCLUSION: Nanoencapsulated carvedilol permeated by a controlled and safe way by SCC4 cell monolayer. SCC4 cells monolayers may be used as in vitro model for sublingual drug transport studies in the development of novel formulations. PMID: 30230390 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Influence of punch geometry (head-flat diameter) and tooling type ('B' or 'D') on the physical-mechanical properties of formulation tablets.
Authors: Shah HG, Dugar RP, Li H, Dave VS, Dave RH Abstract The presented study assessed the influence of punch geometry (head-flat diameter) and tooling type ('B' or 'D') on the physical-mechanical properties of tablets prepared by direct-compression of two guaifenesin (25% or 40% w/w) formulations. Tablets of both formulations were prepared on instrumented, single-layer, rotary tablet press using 10 mm, flat-faced, 'B' or 'D'-type tooling with different head-flat (HF) diameters, and compression forces (CF) ranging from 5-25 KN with 5 KN increments. The tablets were evaluated for dimensions, w...
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Assessment of lisdexamfetamine dimesylate stability and identification of its degradation product by NMR spectroscopy.
Authors: Carlos G, Magalhães A, Isler AC, Comiran E, Fröehlich PE Abstract Lisdexamfetamine dimesylate (LDX), a long-acting prodrug stimulant indicated for the treatment of the attention-deficit/hyperactivity disorder (ADHD), was subjected to forced degradation studies by acid and alkaline hydrolysis and the degradation profile was studied. To obtain between 10-30% of degraded product, acid and alkaline conditions were assessed with solutions of 0.01 M, 0.1 M, 0.5 M and 1 M of DCl and NaOD. These solutions were analyzed through 1H NMR spectra. Acid hydrolysis produced no degradation in 0.01 M and 0.1 M...
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Research on the relationship between cephalosporin structure, solution clarity, and rubber closure compatibility using volatile components profile of butyl rubber closures.
CONCLUSIONS: Based on the results of this study, rubber closures with good compatibility for cephalosporins with different side chain structures can be selected rapidly. This experimental strategy not only facilitates the screening of suitable rubber closures more effectively, but also enables the quick determination of volatile components adsorbed by drugs. PMID: 30231654 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Physicochemical Characterization and Thermal Behavior of Hexosomes Containing Ketoconazole as Potential Topical Antifungal Delivery System.
CONCLUSIONS: Physicochemical properties of the hexosomes containing ketoconazole, are important for topical mycosis treatment administration, conditions of storage, and for its incorporation into formulation of semi-solid dosage forms. PMID: 30231655 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

The Utility of 3D-Printed Airway Stents to Improve Treatment Strategies for Central Airway Obstructions.
Authors: Xu J, Ong HX, Traini D, Byrom M, Williamson J, Young PM Abstract Airway stents are commonly used in the management of patients suffering from central airway obstruction (CAO). CAO may occur directly from airway strictures, obstructing airway cancers, airway fistulas or tracheobronchomalacia, resulting from weakening and dynamic collapse of the airway wall. Current airway stents are constructed from biocompatible medical-grade silicone or from a nickel-titanium (nitinol) alloy with fixed geometry. The stents are inserted via the mouth during a bronchoscopic procedure. Existing stents have many shortcomings ...
Source: Drug Development and Industrial Pharmacy - September 14, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Proof-of-Concept Preparation and Characterization of Dual-Drug Amorphous Nanoparticle Complex as Fixed-Dose Combination of Poorly Soluble Drugs.
CONCLUSION: Dual-drug nanoplex was successfully prepared with high degree of control over its physical characteristics. Nevertheless, whether dual-drug nanoplex always exhibits diminished solubility enhancement compared to its single-drug counterparts needs to be investigated using different poorly-soluble drugs. PMID: 30196726 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 11, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Low molecular weight chitosan based conjugates for efficient Rhein oral delivery: synthesis, characterization, and pharmacokinetics.
CONCLUSION: The present work demonstrated that the RH-LMWC conjugates exhibited sustained release properties with outstanding oral bioavailability enhancements compared to administration of RH itself. Potentially, RH-LMWC conjugates may serve as a promising lead for developing a new platform for RH oral delivery. PMID: 30196732 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 11, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Targeted Thrombolysis by Using c-RGD-modified N,N,N-Trimethyl Chitosan Nanoparticles Loaded with Lumbrokinase.
This study develops a potential thrombolytic therapy by fabricating N,N,N-Trimethyl Chitosan (TMC) nanoparticles modified with the cyclic Arg-Gly-Asp-Phe-Lys peptide (c-RGD) and loaded with LK (i.e., c-RGD-LK-NPs). The binding of c-RGD to platelet membrane GPIIb/IIIa receptors is expected to enable targeted delivery of the c-RGD-conjugated TMC to the thrombus. The synthesized c-RGD-LK-NPs had a mean particle size of 232.0 nm, zeta potential of 19.8mV, entrapment efficiency of 52.7% ± 2.5%, and loading efficiency of 17.4% ± 0.65%. Transmission electron microscopy showed that they were generally spherica...
Source: Drug Development and Industrial Pharmacy - September 11, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development and in vitro characterization of chitosan-coated polymeric nanoparticles for oral delivery and sustained release of the immunosuppressant drug mycophenolate mofetil.
CONCLUSION: Two chitosan-coated nanoparticles formulations of MMF had high EE and a desirable sustained drug release profile in the effort to design a once-daily dosage form for MMF. PMID: 30169982 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - September 1, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Inhibitory Effect of Resveratrol on the Pharmacokinetic of Ibrutinib by UPLC-MS/MS.
CONCLUSIONS: Resveratrol inhibits the pharmacokinetic of ibrutinib in vitro and in vivo. It is necessary to pay more attention to adjust the dose of the drug when resveratrol is used in combination with ibrutinib. PMID: 30156133 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 31, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Fabrication of rosuvastatin-loaded polymeric nanocapsules: A promising modality for treating hepatic cancer delineated by apoptotic and cell cycle arrest assessment.
Authors: Aldalaen S, El-Gogary RI, Nasr M Abstract Nanotechnology has provided several advantages for the treatment of cancer. Polymeric nanocapsules (PNCs) were proven promising in the treatment of different cancer types, such as hepatic cancer. Meanwhile, the exploration of novel indications of old molecules with the purpose of cancer treatment has been widely reported. Among the promising therapeutic moieties, rosuvastatin (RV) was delineated as a potential anticancer drug. Hence, the target of the presented manuscript was to develop PNCs loaded with RV to overcome its delivery challenges and augment its antican...
Source: Drug Development and Industrial Pharmacy - August 25, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development of hydrophilic Gels containing Coenzyme Q10-loaded Liposomes: Characterization, Stability and Rheology measurements.
Authors: Dragicevic N, Krajisnik D, Milic J, Fahr A, Maibach H Abstract OBJECTIVE: The aim of this study was to develop, characterize and evaluate stability of a gel containing coenzyme Q10 (Q10)-loaded liposomes, and enhance the stability of Q10 in the nanocarrier-containing gel compared to the conventional gel. METHODS: Q10-loaded liposome dispersions prepared from unsaturated or saturated lecithin, were characterized for particle size, polydispersity index (PDI), zeta-potential, pH value, oxidation index, Q10-content and morphology, and incorporated into carbomer gel. Liposome gels and liposome-free gel were...
Source: Drug Development and Industrial Pharmacy - August 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Application of liquisolid technology for promoting the renoprotective efficacy of walnut extracts in chronic renal failure rat model.
Authors: Al-Okbi SY, Mohamed DA, Hamed TE, Abd El-Alim SH, Kassem AA, Mostafa DM Abstract Chronic renal failure (CRF) is among the major health problems that could lead to increased morbidity and mortality among population. "Nutraceuticals" is an emerging field for natural agents from plant foods that could reduce the progression of such disease. Many newly developed drugs are having bioavailability problems owing to their water insolubility. Liquisolid technique is one of the promising technological approaches to increase solubility and hence, drug absorption. The aim of the present research was to prepa...
Source: Drug Development and Industrial Pharmacy - August 24, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Inhalable liposomes of Glycyrrhiza glabra extract for use in tuberculosis: Formulation, in vitro characterization, in vivo lung deposition and in vivo pharmacodynamic studies.
CONCLUSION: Licorice extract LDPI thus has a promising potential to be explored as an effective anti-tubercular medicine or as an adjunct to existing anti-tubercular drugs. PMID: 30122088 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 21, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Synthesis and Characterization of Photocatalytic Polyurethane and Poly(Methyl Methacrylate) Microcapsules for the Controlled Release of Methotrexate.
Authors: Al-Nemrawi NK, Marques J, Tavares CJ, Oweis RJ, Al-Fandi MG Abstract The aim of this work is to prepare ultraviolet (UV) triggered controlled release of compounds from microcapsule systems (MCs). Polyurethane (PU) and poly(methyl methacrylate) (PMMA) microcapsules were studied with/without chemical functionalization using photocatalytic TiO2 nanoparticles (NPs) on their surface. Once TiO2 nanoparticles are illuminated with UV light (λ = 370nm) they initiate the rupture of the polymeric bonds of the microcapsule and subsequently initiate the encapsulated compound release, methotrexate (MTX) or rhodam...
Source: Drug Development and Industrial Pharmacy - August 18, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Overcoming drug-resistant lung cancer by paclitaxel-loaded hyaluronic acid-coated liposomes targeted to mitochondria.
Authors: Tian Y, Zhang H, Qin Y, Li D, Liu Y, Wang H, Gan L Abstract As a major cause for the inefficiency of cancer chemotherapy, multidrug resistance (MDR) has become a major barrier to cancer treatment. Mitochondrion-orientated transportation of smart liposomes has been developed as a promising strategy to deliver anticancer drugs directly to tumor sites and actively target the mitochondria, so that drugs can interfere with mitochondrial function and facilitate cell apoptosis, overcoming MDR. Herein, we report a novel dual-functional paclitaxel (PTX) liposome system possessing both CD44 targeting and mitochondri...
Source: Drug Development and Industrial Pharmacy - August 18, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Pharmaceutical excipients properties and screw feeder performance in continuous processing lines: a Quality by Design (QbD) approach.
Authors: Santos BAMC, Almada do Carmo F, Schlindwein W, Muirhead G, Rodrigues CR, Cabral LM, Westrup J, Pitt K Abstract Screw feeder performance is a critical aspect in continuous manufacturing processes. Pharmaceutical excipients, such as mannitol, microcrystalline cellulose, lactose monohydrate and anhydrous dibasic calcium phosphate can present problems in ensuring a continuous stable feed rate due to their sub-optimal flow properties. In alignment with Quality by Design (QbD) goals, the aim of this work was to identify and explain critical sources of variability of some powder excipients delivery by screw feedi...
Source: Drug Development and Industrial Pharmacy - August 18, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Scavenger Receptor Class BI (SR-BI) Mediates Uptake of CPX-351 into a K562 Leukemia Cells.
Authors: Di Y, Wasan EK, Cawthray J, Wasan KM Abstract PURPOSE: CPX-351 is a liposomal formulation of cytarabine and daunorubicin encapsulated at a 5:1 molar ratio, for the treatment of acute myeloid leukemia. The Scavenger Receptor class B type I (SR-BI) plays an important role in mediating the uptake of high-density lipoproteins. The purpose of this study is to assess the role of the cell surface lipoprotein receptor SR-BI in the uptake of CPX-351 liposomes (Jazz Pharmaceuticals) into K562 leukemia cells. METHODS: K562 cells were pre-treated with 10 nM siRNA for 48 hours and then treated with va...
Source: Drug Development and Industrial Pharmacy - August 18, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

All the players in the game: driving home the global commitment for legitimate drugs.
Authors: Babyar J Abstract Substandard, falsified and counterfeit medications are a concern for the industry and for the public's health. Data collection and research on these illegitimate drugs must continue to be a priority and common recommendations must be implemented immediately. The health of the public continues to be at risk, and as such global consensus and collaboration must be swift. Process improvements and policy decisions can support expert recommendations while technology and research continue to drive home change. Addressing counterfeit and substandard drugs is cost effective, feasible and the right...
Source: Drug Development and Industrial Pharmacy - August 18, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Determination of precipitation inhibitory potential of polymers from amorphous solid dispersions.
CONCLUSION: The outcome of the study concluded that SHC can be a promising parameter in screening of polymers for the development of the ASDs. PMID: 30102080 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 15, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Novel Small Self-Assembled Resveratrol -Bearing Cubosomes and Hexosomes: Preparation, Charachterization and Ex Vivo Permeation.
Authors: Badie HA, Abbas H Abstract The study aims to elaborate novel self-assembled liquid crystalline nanoparticles (LCNPs) of resveratrol which has neuro-protective, anti-aging, anticancer activity. Resveratrol loaded LCNPs fabrication and optimization for transdermal delivery was assessed via a quality by design approach based on 23 full factorial designs. The cubic phase of LCNPs was successfully prepared using GMO (glyceryl monooleate) via the emulsification technique. Based on the factorial design, the independent operating variables significantly affected the five dependent responses. The cubosomes and hexo...
Source: Drug Development and Industrial Pharmacy - August 11, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Modification of α-lactose monohydrate as a direct compression excipient using roller compaction.
Modification of α-lactose monohydrate as a direct compression excipient using roller compaction. Drug Dev Ind Pharm. 2018 Aug 10;:1-40 Authors: Abu Fara D, Rashid I, Al-Khamees K, Al-Omari M, Chowdhry BZ, Badwan A Abstract Roller compaction was used to prepare a direct compressed lactose excipient using crystalline α-lactose monohydrate. The effect of various roller compaction process parameters (compaction pressure, compaction repetition, and speed ratio) on the characteristics of compacted α-lactose monohydrate were investigated. The results were compared to the data obtained using ...
Source: Drug Development and Industrial Pharmacy - August 11, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Fabrication and Characterization of Matrix Type Transdermal Patches Loaded With Tizanidine Hydrochloride: Potential Sustained Release Delivery System.
CONCLUSION: The results demonstrated that topically applied transdermal patch will be a potential medicated sustain release patch for muscle pain which will improve patient compliance. PMID: 30081679 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 8, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development and pharmacokinetic evaluation of alginate-pectin polymeric rafts forming tablets using box behnken design.
CONCLUSION: Raft forming system successfully delivered the drug in controlled manner and improved the bioavailability of drugs. PMID: 30084289 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 8, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Physical Barrier Type Abuse-Deterrent Formulations: Monitoring Sintering-Induced Microstructural Changes in Polyethylene Oxide Placebo Tablets by Near Infrared Spectroscopy (NIRS).
CONCLUSIONS: The MSC algorithm was presented to quickly calculate spectral slopes and intercepts for use in SSR and SIR analysis. SSR models were successfully applied and assessed as the optimal modeling technique to monitor sintering of PEO based matrix tablets. PMID: 30070152 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 7, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Investigation of different types of nano drug delivery systems of Atorvastatin for the treatment of Hyperlipidemia.
Authors: Mathur M, Vemula KD Abstract Different nanoparticles namely solid lipid nanoparticles, nanocrystals and nanosponges loaded with atorvastatin were successfully fabricated with desirable technological properties which reckoned promising methods of their preparation. Further, suitable characterization and evaluation parameters for in-vitro and in-vivo studies were conducted which led to increase in drug's bioavailability, provided better in-vivo efficacy and reduced toxicity in treating hyperlipidemia systemically. Particle sizes were found to be less than 300nm, with minimal polydispersity indices and maximi...
Source: Drug Development and Industrial Pharmacy - August 7, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Preparation, characterization and in vitro anticancer activity of paclitaxel conjugated magnetic nanoparticles.
In this study, magnetic nanoparticles (MNPs) coated with L-aspartic acid (F-Asp NPs) were synthesized via a co-precipitation method and conjugated with paclitaxel (PTX) (F-Asp-PTX NPs) by esterification reaction between the carboxylic acid end groups on MNPs surface and the hydroxyl groups of the PTX and studied its cytotoxic effect in vitro. The successful conjugating of PTX onto the nanoparticles (NPs) was confirmed by X-ray diffraction (XRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), vibrating sample magnetometer (VSM) and transmission elec...
Source: Drug Development and Industrial Pharmacy - August 7, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

A novel honokiol liposome: formulation, pharmacokinetics and antitumor studies.
Authors: Zhou C, Guo C, Li W, Zhao J, Yang Q, Tan T, Wan Z, Dong J, Song X, Gong T Abstract It is necessary to discover a novel antitumor liposome with prolonged circulation time, high efficacy and low cost. Here, we reported a liposomal honokiol (HNK) prepared with a new type of excipient, Kolliphor HS15, which was termed as HS15-LP-HNK. In addition, we employed PEGylated liposomal honokiol (PEG-LP-HNK) as positive control. The HS15-LP-HNK was prepared by thin-film hydration method. It was near-spherical morphology with an average size of 80.62 ± 0.72 nm (PDI = 0.234 ± 0.007) and...
Source: Drug Development and Industrial Pharmacy - August 1, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Design and Optimization of Gastric Floating Sustained-Release Mini-tablets of Alfuzosin Hydrochloride Based on a Factorial Design: In vitro/In vivo Evaluation.
Authors: Gong L, Yu M, Sun Y, Gao Y, An T, Zou M, Cheng G Abstract The purpose of this research was to develop multiple-unit gastric floating mini-tablets and to evaluate the possibility of using these mini-tablets as a delivery system to improve the drug absorption for drugs with a narrow absorption window. Mini-tablets were prepared using Hydroxypropyl methylcellulose (HPMC K100M) and carbopol 971P as release retarding agents and sodium bicarbonate (NaHCO3) as gas-forming agent. The properties of the prepared mini-tablets in terms of floating characteristic parameters and in vitro release were evaluated. Furtherm...
Source: Drug Development and Industrial Pharmacy - August 1, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Formulation, Optimization and Characterization of Rifampicin Loaded Solid Lipid Nanoparticles for the Treatment of Tuberculosis.
Authors: Chokshi NV, Khatri HN, Patel MM Abstract Mycobacterium tuberculosis, being the causative infectious agent, is the leading cause of death worldwide amongst the infectious disease. The low bioavailability of rifampicin (RIF), one of the vital constituent of anti-tubercular therapy, instigates an urge to develop nanocarrier, which can prevent its degradation in the acidic pH of the stomach. Solid lipid nanoparticles (SLNs) have been proven to be promising versatile platform for oral delivery of lipophilic drugs. Therefore, the current investigation demonstrates development of rifampicin loaded solid lipid nan...
Source: Drug Development and Industrial Pharmacy - August 1, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

A single subcutaneous administration of a sustained-release ivermectin suspension eliminates Psoroptes cuniculi infection in a rabbit farm.
CONCLUSIONS: A single subcutaneous administration of the IVM-SD suspension at 2 mg/kg was effective in eliminating P. cuniculi infection in the rabbit farm. PMID: 30058406 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 1, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Preparation of curcumin-hydroxypropyl- β-cyclodextrin inclusion complex by cosolvency-lyophilization procedure to enhance oral bioavailability of the drug.
CONCLUSIONS: The CUR-HP-β-CD can be successfully prepared by a simple method, which may be feasible for industrial scaling up, to remarkably increase drug water solubility and oral bioavailability while maintaining its bioactivity and may be a promising therapeutic preparation. PMID: 30059244 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 1, 2018 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research