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Oral Bioavailability Enhancement Of Raloxifene With Nanostructured Lipid Carriers
A. Murthy, Punna Rao Ravi, Himanshu Kathuria, Shrinivas Malekar
Published 2020 · Chemistry, Medicine
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Raloxifene hydrochloride (RLX) shows poor bioavailability (<2%), high inter-patient variability and extensive gut metabolism (>90%). The objective of this study was to develop nanostructured lipid carriers (NLCs) for RLX to enhance its bioavailability. The NLC formulations were produced with glyceryl tribehenate and oleic acid. The particle characteristics, entrapment efficiency (EE), differential scanning calorimetry (DSC), in vitro drug release, oral bioavailability (in rats) and stability studies were performed. The optimized nanoparticles were 120 ± 3 nm in size with positive zeta potential (14.4 ± 0.5 mV); % EE was over 90% with the drug loading of 5%. The RLX exists in an amorphous form in the lipid matrix. The optimized RLX-NLC formulation showed sustained release in vitro. The RLX-NLC significantly (p < 0.05) enhanced oral bioavailability 3.19-fold as compared to RLX-free suspension in female Wistar rats. The RLX-NLC can potentially enhance the oral bioavailability of RLX. It can also improve the storage stability.
This paper references
Development and Evaluation of Solid Lipid Nanoparticles of Raloxifene Hydrochloride for Enhanced Bioavailability
Anand Kumar Kushwaha (2013)
Characterization and in vitro assessment of paclitaxel loaded lipid nanoparticles formulated using modified solvent injection technique.
D. Pandita (2009)
Preparation and characterization of minoxidil loaded nanostructured lipid carrier gel for effective treatment of alopecia.
S. Uprit (2013)
Fate of polymeric nanocarriers for oral drug delivery
L. Plapied (2011)
An Atlas of Osteoporosis: The Encyclopedia of Visual Medicine Series
R. Francis (1993)
Physical chemical considerations of lipid-based oral drug delivery--solid lipid nanoparticles.
P. Bummer (2004)
Proliposome powders for enhanced intestinal absorption and bioavailability of raloxifene hydrochloride: effect of surface charge
Ashok Velpula (2013)
Enhanced bioavailability of raloxifene hydrochloride via dry suspensions prepared from drug/HP-β-cyclodextrin inclusion complexes.
R. Lu (2015)
Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations.
R. Mueller (2002)
Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery
E. B. Soutoa (2004)
Lipid nanoparticle-mediated siRNA delivery for safe targeting of human CML in vivo
N. Jyotsana (2019)
Design, Optimization and Characterization of Nanostructured Lipid Carriers of Raloxifene Hydrochloride for Transdermal Delivery
Durga Puro (2020)
Breast Cancer Characteristics and Survival among Users versus Nonusers of Raloxifene
P. Pinsky (2019)
Development of raloxifene-solid dispersion with improved oral bioavailability via spray-drying technique
T. H. Tran (2013)
Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery
S. Das (2010)
Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.
R. Mueller (2006)
Raloxifene Loaded SLN and NLC: Comparison of In Vitro Properties and In Vivo Behavior after Oral Administration in Rats
A. N. Himanshu Kathuria (2013)
Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: Design and in vivo study.
N. Shah (2016)
Current State-of-Art and New Trends on Lipid Nanoparticles (SLN and NLC) for Oral Drug Delivery
P. Severino (2012)
Formulation optimization and in vitro skin penetration of spironolactone loaded solid lipid nanoparticles.
H. Kelidari (2015)
Solid lipid nanoparticles as drug carriers. I. Incorporation and retention of the lipophilic prodrug 3′-azido-3′-deoxythymidine palmitate
H. Heiati (1997)
Physically Optimized Nano-Lipid Carriers Augment Raloxifene and Vitamin D Oral Bioavailability in Healthy Humans for Management of Osteoporosis.
K. Hosny (2020)
Lipid nanoparticles for oral delivery of raloxifene: optimization, stability, in vivo evaluation and uptake mechanism.
P. R. Ravi (2014)
Glucose-Based Mesoporous Carbon Nanospheres as Functional Carriers for Oral Delivery of Amphiphobic Raloxifene: Insights into the Bioavailability Enhancement and Lymphatic Transport
Yanghuan Ye (2015)
Formulation and optimization of raloxifene-loaded solid lipid nanoparticles to enhance oral bioavailability.
T. H. Tran (2014)
Size-exclusive effect of nanostructured lipid carriers on oral drug delivery.
Huipeng Li (2016)
20 Years of Lipid Nanoparticles (SLN & NLC): Present State of Development & Industrial Applications
R. Mueller (2011)
Selective estrogen receptor modulators: Mechanism of action and clinical experience
D. Thiebaud (2001)
Treatment of Established Postmenopausal Osteoporosis with Raloxifene: A Randomized Trial
E. Lufkin (1998)
Assessment of Osteoporosis at the Primary Health Care Level; Technical Report; World Health Organization Collaborating Centre for Metabolic Bone Diseases
J. Kanis (2008)
Solid lipid nanoparticles of mitoxantrone for local injection against breast cancer and its lymph node metastases.
B. Lu (2006)
Formulation and characterization of lipid-based drug delivery system of raloxifene-microemulsion and self-microemulsifying drug delivery system
H. Thakkar (2011)
Encapsulation of Vitamin A Palmitate in Nanostructured Lipid Carrier (NLC)-Effect of Surfactant Concentration on the Formulation Properties.
Akram Pezeshki (2014)
A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability
G. Amidon (2004)
Influence of hepatic and intestinal efflux transporters and their genetic variants on the pharmacokinetics and pharmacodynamics of raloxifene in osteoporosis treatment.
Tina Trdan Lušin (2012)
Drug Delivery Markets—An Outlook
S. M. Findlay (2016)
Role of nanoparticle size, shape and surface chemistry in oral drug delivery.
Amrita Banerjee (2016)
Size-dependent lymphatic uptake of nanoscale-tailored particles as tumor mass increases
P. Kjellman (2015)
Absorption, pharmacokinetics and disposition properties of solid lipid nanoparticles (SLNs).
Jing Wang (2012)
Evaluation of oral bioavailability and anticancer potential of raloxifene solid lipid nanoparticles.
Somashekhar Battani (2014)
Preparation and evaluation of raloxifene-loaded solid dispersion nanoparticle by spray-drying technique without an organic solvent.
T. H. Tran (2013)
Lipid-based delivery systems and intestinal lymphatic drug transport: A mechanistic update☆
Natalie L Trevaskis (2008)
Oral Nanoparticles Exhibit Specific High-Efficiency Intestinal Uptake and Lymphatic Transport.
K. Kim (2018)
Development, validation, and pharmacokinetic application of liquid chromatographic method for estimation of raloxifene hydrochloride in rabbit plasma
P. R. Ravi (2012)
20 years of lipid nanoparticles (SLN and NLC): present state of development and industrial applications.
R. Mueller (2011)
An estimate of the worldwide prevalence and disability associated with osteoporotic fractures
O. Johnell (2006)
Body distribution in mice of intravenously injected camptothecin solid lipid nanoparticles and targeting effect on brain.
S. Yang (1999)
Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives
Melike Üner (2007)
Selective estrogen receptor modulators: mechanism of action and clinical experience. Focus on raloxifene.
D. Thiebaud (2001)
Effect of poloxamer 188 on lymphatic uptake of carvedilol-loaded solid lipid nanoparticles for bioavailability enhancement
Baboota Sanjula (2009)
Skeletal and nonskeletal effects of raloxifene
O. Gluck (2003)
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